DGIdb - BRAF Gene Record

BRAF 673 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

673
B-RAF PROTO-ONCOGENE, SERINE/THREONINE KINASE
BRAF
B-RAF1
B-raf
BRAF1
NS7
RAFB1
164757
1097
ENSG00000157764
OTTHUMG00000157457
P15056
PA25408
v-raf murine sarcoma viral oncogene homolog B1
B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (P94) (V-RAF MURINE SARCOMA VIRAL ONCOGENE HOMOLOG B1). [SOURCE:UNIPROT/SWISSPROT;ACC:P15056]
p94
Proto-oncogene B-Raf
Serine/threonine-protein kinase B-raf
1943
NP_004324
NM_004333
5
BE0000634
BRAF1_HUMAN
BRAF_HUMAN
RAF
T99089

Gene Info:

Target Class	Enzymes
Target Subclass	EC:2.7.11.1
Human Readable Name	DRUGGABLE GENOME
GuideToPharmacology Gene Category Name	RAF family
GuideToPharmacology Gene Category ID	610
Target Subclass	2.7.11.1
Target Main Class	Enzymes
CancerCommons Reported Gene Name	BRAF (V660) E/K
CancerCommons Reported Gene Name	BRAF
CancerCommons Reported Gene Name	Pan-RAF
CancerCommons Reported Gene Name	BRAF V600E
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR001245
Uniprot Status	Swiss-Prot
Interpro Type	Domain
Human Readable Name	KINASE
Gene Biotype	PROTEIN_CODING

(29 More Sources)

Gene Categories: Category Details

KINASE
SERINE THREONINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME

Publications:

Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
Greger et al., 2012, Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations., Mol. Cancer Ther.
Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
Okimoto RA et al., 2016 Nov 22, Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer., Proc Natl Acad Sci U S A
Basile et al., 2014, Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors., Pigment Cell Melanoma Res
Dienstmann et al., 2015, Database of genomic biomarkers for cancer drugs and clinical targetability in solid tumors., Cancer Discov
Nicolaides et al., 2011, Targeted therapy for BRAFV600E malignant astrocytoma., Clin. Cancer Res.
Hoftijzer et al., 2009, Beneficial effects of sorafenib on tumor progression, but not on radioiodine uptake, in patients with differentiated thyroid carcinoma., Eur. J. Endocrinol.
Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
Villanueva et al., 2010, Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K., Cancer Cell
Tiacci et al., 2011, BRAF mutations in hairy-cell leukemia., N. Engl. J. Med.
Sosman et al., 2012, Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib., N. Engl. J. Med.
Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
Rizzo et al., 2010, Prognostic vs predictive molecular biomarkers in colorectal cancer: is KRAS and BRAF wild type status required for anti-EGFR therapy?, Cancer Treat. Rev.
Lovly et al., 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS ONE
Falchook et al., 2013, BRAF mutant gastrointestinal stromal tumor: first report of regression with BRAF inhibitor dabrafenib (GSK2118436) and whole exomic sequencing for analysis of acquired resistance., Oncotarget
Mao et al., 2013, Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents., Clin. Cancer Res.
Chen et al., 2014, BRAFV600E mutation and its association with clinicopathological features of colorectal cancer: a systematic review and meta-analysis., PLoS ONE
Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
Huillard et al., 2012, Cooperative interactions of BRAFV600E kinase and CDKN2A locus deficiency in pediatric malignant astrocytoma as a basis for rational therapy., Proc. Natl. Acad. Sci. U.S.A.
Peeters et al., 2013, Massively parallel tumor multigene sequencing to evaluate response to panitumumab in a randomized phase III study of metastatic colorectal cancer., Clin. Cancer Res.
Nagore et al., 2014, Prognostic value of BRAF mutations in localized cutaneous melanoma., J. Am. Acad. Dermatol.
Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
McArthur et al., 2014, Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study., Lancet Oncol.
Mao et al., 2011, BRAF V600E mutation and resistance to anti-EGFR monoclonal antibodies in patients with metastatic colorectal cancer: a meta-analysis., Mol. Biol. Rep.
De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
Haldar et al., 2011, Epidermal growth factor receptor blockers for the treatment of ovarian cancer., Cochrane Database Syst Rev
Penna et al., 2016, Primary cross-resistance to BRAFV600E-, MEK1/2- and PI3K/mTOR-specific inhibitors in BRAF-mutant melanoma cells counteracted by dual pathway blockade., Oncotarget
Corcoran et al., 2012, EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib., Cancer Discov
Xing et al., 2014, BRAF V600E and TERT promoter mutations cooperatively identify the most aggressive papillary thyroid cancer with highest recurrence., J. Clin. Oncol.
Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
Faber et al., 2014, mTOR inhibition specifically sensitizes colorectal cancers with KRAS or BRAF mutations to BCL-2/BCL-XL inhibition by suppressing MCL-1., Cancer Discov
Agaimy et al., 2009, V600E BRAF mutations are alternative early molecular events in a subset of KIT/PDGFRA wild-type gastrointestinal stromal tumours., J. Clin. Pathol.
De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.
Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.
Kirkwood et al., 2012, Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma., Clin. Cancer Res.
Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
Nissan et al., 2014, Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence., Cancer Res.
Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
Jalili et al., 2012, Dual suppression of the cyclin-dependent kinase inhibitors CDKN2C and CDKN1A in human melanoma., J. Natl. Cancer Inst.
Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
Rudin et al., 2013, Molecular characterization of acquired resistance to the BRAF inhibitor dabrafenib in a patient with BRAF-mutant non-small-cell lung cancer., J Thorac Oncol
Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
Boulalas et al., Mutational analysis of the BRAF gene in transitional cell carcinoma of the bladder., Int. J. Biol. Markers
Sarker et al., 2015, First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors., Clin. Cancer Res.
Crescenzi et al., 2014, Immunohistochemistry for BRAF(V600E) antibody VE1 performed in core needle biopsy samples identifies mutated papillary thyroid cancers., Horm. Metab. Res.
Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov
Rubinstein et al., 2010, Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032., J Transl Med
Kim et al., 2013, Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation., Thyroid
Dienstmann et al., 2011, BRAF as a target for cancer therapy., Anticancer Agents Med Chem
Chapman et al., 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med.
Tol et al., 2010, Markers for EGFR pathway activation as predictor of outcome in metastatic colorectal cancer patients treated with or without cetuximab., Eur. J. Cancer
Ji et al., 2013, Vemurafenib synergizes with nutlin-3 to deplete survivin and suppresses melanoma viability and tumor growth., Clin. Cancer Res.
Morris et al., 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov
Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
Patel et al., 2013, Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma., Cancer
He et al., 2014, Prognostic value of the BRAF V600E mutation in papillary thyroid carcinoma., Oncol Lett
Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
Zecchin et al., 2013, BRAF V600E is a determinant of sensitivity to proteasome inhibitors., Mol. Cancer Ther.
Hayes et al., 2012, Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements., Clin. Cancer Res.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Meckbach et al., 2014, BRAF-V600 mutations have no prognostic impact in stage IV melanoma patients treated with monochemotherapy., PLoS ONE
Ascierto et al., 2013, Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma., J. Clin. Oncol.
De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.
Walczyk et al., 2014, The BRAF(V600E) mutation in papillary thyroid microcarcinoma: does the mutation have an impact on clinical outcome?, Clin. Endocrinol. (Oxf)
Howell et al., 2011, Both BRAF V600E mutation and older age (≥ 65 years) are associated with recurrent papillary thyroid cancer., Ann. Surg. Oncol.
Wan et al., 2004, Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF., Cell
Flaherty et al., 2012, Improved survival with MEK inhibition in BRAF-mutated melanoma., N. Engl. J. Med.
Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
Kurman et al., 2011, Molecular pathogenesis and extraovarian origin of epithelial ovarian cancer--shifting the paradigm., Hum. Pathol.
Falchook et al., 2012, Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial., Lancet Oncol.
Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Rowland et al., 2015, Meta-analysis of BRAF mutation as a predictive biomarker of benefit from anti-EGFR monoclonal antibody therapy for RAS wild-type metastatic colorectal cancer., Br. J. Cancer
Flaherty et al., 2010, Inhibition of mutated, activated BRAF in metastatic melanoma., N. Engl. J. Med.
Ohashi et al., 2012, Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1., Proc. Natl. Acad. Sci. U.S.A.
Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
Jordan et al., 2012, Vemurafenib for the treatment of melanoma., Expert Opin Pharmacother
Shi H et al., 2014, Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy., Cancer Discov
Hoogstraat et al., 2015, Detailed imaging and genetic analysis reveal a secondary BRAF(L505H) resistance mutation and extensive intrapatient heterogeneity in metastatic BRAF mutant melanoma patients treated with vemurafenib., Pigment Cell Melanoma Res
Wagenaar et al., 2014, Resistance to vemurafenib resulting from a novel mutation in the BRAFV600E kinase domain., Pigment Cell Melanoma Res
Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov
Sahadudheen et al., 2016, Long Term Survival and Continued Complete Response of Vemurafenib in a Metastatic Melanoma Patient with BRAF V600K Mutation., Case Rep Oncol Med
Bahadoran et al., 2013, Major clinical response to a BRAF inhibitor in a patient with a BRAF L597R-mutated melanoma., J. Clin. Oncol.
Hutchinson et al., 2013, BRAF fusions define a distinct molecular subset of melanomas with potential sensitivity to MEK inhibition., Clin. Cancer Res.
Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol
Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol
Hyman et al., 2015, Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations., N. Engl. J. Med.
Hainsworth JD et al., 2018, Targeted Therapy for Advanced Solid Tumors on the Basis of Molecular Profiles: Results From MyPathway, an Open-Label, Phase IIa Multiple Basket Study., J Clin Oncol
Silkin SV et al., 2016, Complete Clinical Response of BRAF-Mutated Cholangiocarcinoma to Vemurafenib, Panitumumab, and Irinotecan., J Gastrointest Cancer
Hong et al., 2016, Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation., Cancer Discov
Sharman et al., 2014, Vemurafenib response in 2 patients with posttransplant refractory BRAF V600E-mutated multiple myeloma., Clin Lymphoma Myeloma Leuk
Brose et al., 2016, Vemurafenib in patients with BRAF(V600E)-positive metastatic or unresectable papillary thyroid cancer refractory to radioactive iodine: a non-randomised, multicentre, open-label, phase 2 trial., Lancet Oncol.
Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov
Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
Ali et al., 2014, Extended Antitumor Response of a BRAF V600E Papillary Thyroid Carcinoma to Vemurafenib., Case Rep Oncol
Savarese et al., beta-Adrenergic receptor decrease in diabetic rat hearts., Life Sci.
Whittaker et al., 2013, A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition., Cancer Discov
Dietrich et al., 2012, BRAF inhibition in refractory hairy-cell leukemia., N. Engl. J. Med.
Peng et al., 2015, Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers., Cancer Cell
Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
Nazarian et al., 2010, Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation., Nature
Gautschi et al., 2013, Lung adenocarcinoma with BRAF G469L mutation refractory to vemurafenib., Lung Cancer
Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
Peters et al., 2013, Dramatic response induced by vemurafenib in a BRAF V600E-mutated lung adenocarcinoma., J. Clin. Oncol.
Tiacci et al., 2015, Targeting Mutant BRAF in Relapsed or Refractory Hairy-Cell Leukemia., N. Engl. J. Med.
Lin et al., 2015, The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies., Nat. Genet.
Joshi et al., 2015, Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer., PLoS ONE
Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
Yao et al., 2015, BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition., Cancer Cell
Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
Peh et al., 2016, The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas., Mol. Cancer Ther.
Shen et al., 2016, Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma., Nat. Med.
Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Kirouac et al., 2017, Clinical responses to ERK inhibition in BRAF(V600E)-mutant colorectal cancer predicted using a computational model., NPJ Syst Biol Appl
Bonnevaux et al., 2016, Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor., Mol. Cancer Ther.
Choi et al., 2014, Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors., Pigment Cell Melanoma Res
Kordes et al., 2016, Cooperation of BRAF(F595L) and mutant HRAS in histiocytic sarcoma provides new insights into oncogenic BRAF signaling., Leukemia
Banerjee et al., 2016, A Rare Finding of a BRAF Mutation in Renal Cell Carcinoma with Response to BRAF-Directed Targeted Therapy., Cureus
Narita et al., 2014, Novel ATP-competitive MEK inhibitor E6201 is effective against vemurafenib-resistant melanoma harboring the MEK1-C121S mutation in a preclinical model., Mol. Cancer Ther.
Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
Feng et al., 2016, A Novel Plant Sesquiterpene Lactone Derivative, DETD-35, Suppresses BRAFV600E Mutant Melanoma Growth and Overcomes Acquired Vemurafenib Resistance in Mice., Mol. Cancer Ther.
Feng et al., 2015, SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex., Cancer Res.
Montero-Conde et al., 2013, Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas., Cancer Discov
Yaeger et al., 2015, Pilot trial of combined BRAF and EGFR inhibition in BRAF-mutant metastatic colorectal cancer patients., Clin. Cancer Res.
Kopetz et al., 2015, Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer., J. Clin. Oncol.
Connolly et al., 2014, Anticancer activity of combination targeted therapy using cetuximab plus vemurafenib for refractory BRAF (V600E)-mutant metastatic colorectal carcinoma., Curr Oncol
Budina-Kolomets et al., 2016, HSP70 Inhibition Limits FAK-Dependent Invasion and Enhances the Response to Melanoma Treatment with BRAF Inhibitors., Cancer Res.
Yang W et al., 2015, Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors., Eur J Med Chem
Tsai et al., 2008, Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity., Proc. Natl. Acad. Sci. U.S.A.
Donadieu J et al., 2019, Vemurafenib for Refractory Multisystem Langerhans Cell Histiocytosis in Children: An International Observational Study., J Clin Oncol
Ugurel S et al., 2015, A multicenter DeCOG study on predictors of vemurafenib therapy outcome in melanoma: pretreatment impacts survival., Ann Oncol
Selt F et al., 2017, Establishment and application of a novel patient-derived KIAA1549:BRAF-driven pediatric pilocytic astrocytoma model for preclinical drug testing., Oncotarget
Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A
Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
Corcoran RB et al., 2018, Combined BRAF, EGFR, and MEK Inhibition in Patients with <i>BRAF</i><sup>V600E</sup>-Mutant Colorectal Cancer., Cancer Discov
2016, Triple Therapy Improves Colorectal Cancer Response., Cancer Discov
Yaeger R et al., 2019, Response to Anti-EGFR Therapy in Patients with BRAF non-V600-Mutant Metastatic Colorectal Cancer., Clin Cancer Res
Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
Su et al., 2012, RAF265 inhibits the growth of advanced human melanoma tumors., Clin. Cancer Res.
Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
McNew et al., 2016, MEK and TAK1 Regulate Apoptosis in Colon Cancer Cells with KRAS-Dependent Activation of Proinflammatory Signaling., Mol. Cancer Res.
Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
Beloueche-Babari et al., 2013, Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI., Br. J. Cancer
Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
Fangusaro J et al., 2019, Selumetinib in paediatric patients with BRAF-aberrant or neurofibromatosis type 1-associated recurrent, refractory, or progressive low-grade glioma: a multicentre, phase 2 trial., Lancet Oncol
Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
Lu et al., 2017, Engineering and Functional Characterization of Fusion Genes Identifies Novel Oncogenic Drivers of Cancer., Cancer Res.
Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
Drobysheva et al., 2017, Targeted MAPK Pathway Inhibitors in Patients With Disseminated Pilocytic Astrocytomas., J Natl Compr Canc Netw
Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
Long et al., 2016, Overall Survival and Durable Responses in Patients With BRAF V600-Mutant Metastatic Melanoma Receiving Dabrafenib Combined With Trametinib., J. Clin. Oncol.
Kim et al., 2013, Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor., J. Clin. Oncol.
Marconcini et al., 2017, Metastatic BRAF K601E-mutated melanoma reaches complete response to MEK inhibitor trametinib administered for over 36 months., Exp Hematol Oncol
Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
Long et al., 2014, Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma., N. Engl. J. Med.
Long GV et al., 2017 Sep 10, Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma., N Engl J Med
Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.
Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
Lange et al., 2014, Biological and molecular effects of small molecule kinase inhibitors on low-passage human colorectal cancer cell lines., Biomed Res Int
Waizenegger et al., 2016, A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation., Mol. Cancer Ther.
Agarwal et al., 2016, Response to Targeted Therapy in BRAF Mutant Anaplastic Thyroid Cancer., J Natl Compr Canc Netw
Schreuer et al., 2017, Combination of dabrafenib plus trametinib for BRAF and MEK inhibitor pretreated patients with advanced BRAF(V600)-mutant melanoma: an open-label, single arm, dual-centre, phase 2 clinical trial., Lancet Oncol.
Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
Teh et al., 2016, An In Vivo Reporter to Quantitatively and Temporally Analyze the Effects of CDK4/6 Inhibitor-Based Therapies in Melanoma., Cancer Res.
Isaacson AL et al., 2019, Urothelial carcinoma with an <i>NRF1-BRAF</i> rearrangement and response to targeted therapy., Cold Spring Harb Mol Case Stud
Aguirre AJ et al., 2018, Real-time Genomic Characterization of Advanced Pancreatic Cancer to Enable Precision Medicine., Cancer Discov
Long GV et al., 2014, Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma., Nat Commun
Ross et al., 2016, The distribution of BRAF gene fusions in solid tumors and response to targeted therapy., Int. J. Cancer
Bowyer et al., 2014, Activity of trametinib in K601E and L597Q BRAF mutation-positive metastatic melanoma., Melanoma Res.
Jing et al., 2012, Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212., Mol. Cancer Ther.
Subbiah V et al., 2018, Dabrafenib and Trametinib Treatment in Patients With Locally Advanced or Metastatic BRAF V600-Mutant Anaplastic Thyroid Cancer., J Clin Oncol
Robert et al., 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med.
Planchard et al., 2016, Dabrafenib plus trametinib in patients with previously treated BRAF(V600E)-mutant metastatic non-small cell lung cancer: an open-label, multicentre phase 2 trial., Lancet Oncol.
Müller-Gärtner et al., 1989, [Long-term results following surgery or radioiodine treatment of solitary autonomous adenoma of the thyroid gland]., Chirurg
Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
Mir A et al., 2019, Giant Congenital Melanocytic Nevus Treated With Trametinib., Pediatrics
Jain P et al., 2017, Overcoming resistance to single-agent therapy for oncogenic <i>BRAF</i> gene fusions <i>via</i> combinatorial targeting of MAPK and PI3K/mTOR signaling pathways., Oncotarget
Noeparast A et al., 2016, Non-V600 BRAF mutations recurrently found in lung cancer predict sensitivity to the combination of Trametinib and Dabrafenib., Oncotarget
Lu et al., 2010, Sorafenib induces growth inhibition and apoptosis of human chondrosarcoma cells by blocking the RAF/ERK/MEK pathway., J Surg Oncol
Flaherty, 2006, Chemotherapy and targeted therapy combinations in advanced melanoma., Clin. Cancer Res.
Kim et al., 2007, Sorafenib inhibits the angiogenesis and growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice., Mol. Cancer Ther.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Haluska et al., 2006, Therapeutic targets in melanoma: map kinase pathway., Curr Oncol Rep
Eisen et al., 2006, Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis., Br. J. Cancer
Smalley et al., 2009, CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations., Oncogene
Nakaoku et al., 2014, Druggable oncogene fusions in invasive mucinous lung adenocarcinoma., Clin. Cancer Res.
Palanisamy et al., 2010, Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma., Nat. Med.
Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
Hirschi et al., 2014, Genetic targeting of B-RafV600E affects survival and proliferation and identifies selective agents against BRAF-mutant colorectal cancer cells., Mol. Cancer
Al-Marrawi et al., 2013, Off-label use of cetuximab plus sorafenib and panitumumab plus regorafenib to personalize therapy for a patient with V600E BRAF-mutant metastatic colon cancer., Cancer Biol. Ther.
Mangana et al., 2012, Sorafenib in melanoma., Expert Opin Investig Drugs
Casadei Gardini et al., 2016, Efficacy of sorafenib in BRAF-mutated non-small-cell lung cancer (NSCLC) and no response in synchronous BRAF wild type-hepatocellular carcinoma: a case report., BMC Cancer
Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
Hoeflich et al., 2009, Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression., Cancer Res.
Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol
Bendell et al., 2017, A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor., Br. J. Cancer
Ascierto et al., 2013, MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study., Lancet Oncol.
Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
Tang et al., 2015, BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers., Mol. Cancer Ther.
Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
Di Nicolantonio et al., 2010, Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus., J. Clin. Invest.
Mohseni et al., 2010, PIK3CA and KRAS mutations predict for response to everolimus therapy: now that's RAD001., J. Clin. Invest.
Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
Souglakos J et al., 2009, Prognostic and predictive value of common mutations for treatment response and survival in patients with metastatic colorectal cancer., Br J Cancer
Tol J et al., 2009, BRAF mutation in metastatic colorectal cancer., N Engl J Med
Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov
Garnett et al., 2012, Systematic identification of genomic markers of drug sensitivity in cancer cells., Nature
Casadevall et al., 2016, Dabrafenib in an elderly patient with metastatic melanoma and BRAF V600R mutation: a case report., J Med Case Rep
Planchard et al., 2016, Dabrafenib in patients with BRAF(V600E)-positive advanced non-small-cell lung cancer: a single-arm, multicentre, open-label, phase 2 trial., Lancet Oncol.
Loaiza-Bonilla A et al., 2014, Dramatic response to dabrafenib and trametinib combination in a BRAF V600E-mutated cholangiocarcinoma: implementation of a molecular tumour board and next-generation sequencing for personalized medicine., Ecancermedicalscience
Lavingia V et al., 2016, Impressive response to dual <i>BRAF</i> and MEK inhibition in patients with BRAF mutant intrahepatic cholangiocarcinoma-2 case reports and a brief review., J Gastrointest Oncol
Kocsis J et al., 2017, Combined dabrafenib and trametinib treatment in a case of chemotherapy-refractory extrahepatic BRAF V600E mutant cholangiocarcinoma: dramatic clinical and radiological response with a confusing synchronic new liver lesion., J Gastrointest Oncol
Ponti et al., 2013, The somatic affairs of BRAF: tailored therapies for advanced malignant melanoma and orphan non-V600E (V600R-M) mutations., J. Clin. Pathol.
Gibney et al., 2013, Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies., Expert Opin Drug Metab Toxicol
Garner et al., 1975, Effect of pH on substrate and inhibitor kinetic constants of human liver alanine aminopeptidase. Evidence for two ionizable active center groups., Biochemistry
Poole-Wilson et al., 1975, Effect of pH on ionic exchange and function in rat and rabbit myocardium., Am. J. Physiol.
Fioravanti et al., 1976, Pyridine nucleotide transhydrogenases of parasitic helminths., Arch. Biochem. Biophys.
Bland et al., 1976, Rapid infusion of sodium bicarbonate and albumin into high-risk premature infants soon after birth: a controlled, prospective trial., Am. J. Obstet. Gynecol.
Hargrave DR et al., 2019, Efficacy and Safety of Dabrafenib in Pediatric Patients with <i>BRAF</i> V600 Mutation-Positive Relapsed or Refractory Low-Grade Glioma: Results from a Phase I/IIa Study., Clin Cancer Res
van Geel et al., 2017, A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer., Cancer Discov
Montagut et al., 2012, Identification of a mutation in the extracellular domain of the Epidermal Growth Factor Receptor conferring cetuximab resistance in colorectal cancer., Nat. Med.
Ciardiello et al., 2016, Cetuximab continuation after first progression in metastatic colorectal cancer (CAPRI-GOIM): a randomized phase II trial of FOLFOX plus cetuximab versus FOLFOX., Ann. Oncol.
Hechtman et al., 2015, AKT1 E17K in Colorectal Carcinoma Is Associated with BRAF V600E but Not MSI-H Status: A Clinicopathologic Comparison to PIK3CA Helical and Kinase Domain Mutants., Mol. Cancer Res.
Hsu HC et al., 2016, Mutations of KRAS/NRAS/BRAF predict cetuximab resistance in metastatic colorectal cancer patients., Oncotarget
Loupakis et al., 2009, KRAS codon 61, 146 and BRAF mutations predict resistance to cetuximab plus irinotecan in KRAS codon 12 and 13 wild-type metastatic colorectal cancer., Br. J. Cancer
Shinozaki E et al., 2017, Clinical significance of BRAF non-V600E mutations on the therapeutic effects of anti-EGFR monoclonal antibody treatment in patients with pretreated metastatic colorectal cancer: the Biomarker Research for anti-EGFR monoclonal Antibodies by Comprehensive Cancer genomics (BREAC) study., Br J Cancer
Dietlein et al., 2015, A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer., Cell
Herath et al., 2016, The DNA Repair Inhibitor DT01 as a Novel Therapeutic Strategy for Chemosensitization of Colorectal Liver Metastasis., Mol. Cancer Ther.
Aung et al., 2016, Testing ERBB2 p.L755S kinase domain mutation as a druggable target in a patient with advanced colorectal cancer., Cold Spring Harb Mol Case Stud
Byron et al., 2012, Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status., Mol. Cancer
Tripathy et al., 2017, Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors., Clin. Cancer Res.
Koelblinger P et al., 2018, Development of encorafenib for BRAF-mutated advanced melanoma., Curr Opin Oncol
Moschos SJ et al., 2015, Targeted therapies in melanoma., Surg Oncol Clin N Am
Li Z et al., 2016, Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells., Cancer Lett
Hong et al., 2015, Phase I Dose-Escalation Study of the Multikinase Inhibitor Lenvatinib in Patients with Advanced Solid Tumors and in an Expanded Cohort of Patients with Melanoma., Clin. Cancer Res.
Frederick et al., 2014, Clinical profiling of BCL-2 family members in the setting of BRAF inhibition offers a rationale for targeting de novo resistance using BH3 mimetics., PLoS ONE
Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
Ghosh C et al., 2020, A Combinatorial Strategy for Targeting <i>BRAF</i> <sup>V600E</sup>-Mutant Cancers with BRAF<sup>V600E</sup> Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. Cancer Res.
Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
James et al., 2012, CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity., Mol. Cancer Ther.
Lieu et al., 2015, Antitumor activity of a potent MEK inhibitor, TAK-733, against colorectal cancer cell lines and patient derived xenografts., Oncotarget
Acquaviva et al., 2014, Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib., Mol. Cancer Ther.
LaBonte et al., 2011, The dual EGFR/HER2 inhibitor lapatinib synergistically enhances the antitumor activity of the histone deacetylase inhibitor panobinostat in colorectal cancer models., Cancer Res.
Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
Solit et al., 2006, BRAF mutation predicts sensitivity to MEK inhibition., Nature
Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.
Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
Iverson et al., 2009, RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer., Cancer Res.
Foster et al., 2015, The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models., Mol. Cancer Ther.
Smith et al., 2015, The HSP90 inhibitor ganetespib potentiates the antitumor activity of EGFR tyrosine kinase inhibition in mutant and wild-type non-small cell lung cancer., Target Oncol
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

DABRAFENIB BRAF

Interaction Score: 3.55

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Response Type predicted – resistant

Indication/Tumor Type ovarian cancer

combination therapy AMG 232 + Trametinib + Dabrafenib

PMIDs:
28512244 26392102 26811525 27500726 27659046 27770002 22608338 26732095 27255157 25265492 28891408 24265153 24265154 27080216 27048246 27697975 28784858 28268064 22735384 24885690 27312529 22389471 27797976 25370473 27523909 24265155 25452114 25673644 25265494 23031422 29072975 23020132 29431699 25435907 28078132 28480077 25399551 27283860 24583796 23463675 23621583 25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 22351686 22048237 23833300 24576830 22997239 19238210 23524406 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 21483012 12460919 22743296 12068308 38 2014 8009 2013 8006 2015 31811016 28947956

Sources:
TALC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI DoCM COSMIC CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
VEMURAFENIB BRAF

Interaction Score: 3.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status late trials

Clinical Status early trials

Clinical Status case report

PMIDs:
25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 23094782 24265155 25515853 24112705 22798288 26989536 23715574 24345920 25037139 27480103 26287849 29320312 26687137 27729313 24997557 27460442 27048246 25265494 24987354 231718 23288408 22621641 26343583 28783719 21107323 24035431 24265153 23733758 26352686 25665005 25706985 27760111 25939769 26343582 21383288 26267534 24265152 26732095 27297867 27500726 27523909 28514312 28649441 27196754 24283590 26582644 26918217 24448821 27312529 26137449 27048951 26603897 23365119 25589621 26460303 24523613 26984758 25462267 18287029 31513482 25524477 28002790 23533272

Sources:
TALC DTC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
PANITUMUMAB BRAF

Interaction Score: 2.65

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration MET:amp;BRAF:V600E

Drug family BRAF inhibitor;EGFR mAb inhibitor

combination therapy Vemurafenib;Panitumumab

PMIDs:
23325582 21163703 20619739 28783719 25673644 29431699 26687137 19001320 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 24107445 22241789 26619011 24586605 23918947 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 27770002 27312529 28514312 25589621 31515458

Sources:
JAX-CKB CGI DoCM CIViC OncoKB
TRAMETINIB BRAF

Interaction Score: 1.88

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib + Dabrafenib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
28512244 27338794 28784858 26392102 24265152 26811525 27500726 26343583 27770002 27760111 23248257 28344857 25370473 25706985 26732095 22663011 25265492 28891408 26369631 24265154 24265153 26469692 25309914 26916115 27048246 27697975 27222538 28268064 27297867 25665005 27312529 22389471 27797976 22805292 27488531 22798288 28783719 31010895 29903880 25452114 26314551 24933606 25265494 22169769 24345920 29072975 23020132 29431699 25399551 27283860 24583796 2493360 23715574 25656898 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 23325582 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 20619739 19255327 23031422 22351686 22048237 23833300 24576830 22997239 19238210 23524406 22735384 22281684 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 20368568 19001320 24107445 22241789 26619011 24586605 23918947 21163703 24354346 21594703 15035987 23549875 21683865 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 8006 2015 30792255 29156677 28947956

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI DoCM CIViC PharmGKB FDA OncoKB
CHEMBL525191 BRAF

Interaction Score: 1.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
23549875

Sources:
CIViC GuideToPharmacology
PLX8394 BRAF

Interaction Score: 1.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
27834212 24422853

Sources:
JAX-CKB GuideToPharmacology TTD OncoKB
ENCORAFENIB BRAF

Interaction Score: 1.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources:
TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB
PLX-4720 BRAF

Interaction Score: 1.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources:
DrugBank JAX-CKB CGI CIViC GuideToPharmacology
RAF-265 BRAF

Interaction Score: 1.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Response Type resistant

PMIDs:
20538618 22351689

Sources:
DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons
CETUXIMAB BRAF

Interaction Score: 1.25

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + PLX4720

combination therapy Vemurafenib + Cetuximab

combination therapy Cetuximab + Dabrafenib + SCH772984

PMIDs:
26287849 28363909 28783719 22270724 22281684 24523613 26208524 26916115 27312529 25838391 27002107 25714871 23325582 21163703 20619739 22038996 19773371 23845441 14679157 22180495 21156289 21663470 22356324 12460918 18541894 23406027 21129611 22536370 23470635 23251002 24594804 19018267 22586120 24388723 19010912 24508103 20857202 19537845 21975775 26678033 22448344 25024077 20350999 24163374 19561230 19255327 23031422 22351686 22048237 23833300 24576830 22389471 23020132 22997239 19238210 23524406 22735384 19404918 25370471 24570209 23612012 20630094 23489023 21426297 21639808 20413299 23812671 23614898 22649091 22972589 24396464 24583796 20368568 19001320 24107445 22241789 26619011 24586605 23918947 24354346 21594703 15035987 22663011 23549875 21683865 22805292 23934108 25157968 25989278 20818844 22773810 22608338 21483012 12460919 22743296 12068308 26989027 19603024 27729313 19603018 31566309 19571295 31515458 28972961

Sources:
JAX-CKB CGI DoCM CIViC OncoKB
CHEMBL526479 BRAF

Interaction Score: 1.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
SB590885 BRAF

Interaction Score: 1.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a cell-free assay

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
27523909 20538618

Sources:
JAX-CKB GuideToPharmacology
RG-7256 BRAF

Interaction Score: 1.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CEP-32496 BRAF

Interaction Score: 0.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of wild type BRAF activity.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
22319199

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology TTD
PLX-8394 BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL2144069 BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23398453

Sources:
DTC
LY-3009120 BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
22798288 26732095 26343583

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology
XL-281 BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
DABRAFENIB MESYLATE BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL217354 BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vemurafenib + TW-37

Indication/Tumor Type non-small cell lung carcinoma

Evidence Type Actionable

PMIDs:
25665005

Sources:
JAX-CKB
ZELBORAF BRAF

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

PMIDs:
None found

Sources:
CancerCommons
COBIMETINIB BRAF

Interaction Score: 0.52

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status FDA approved

Approval Status Phase Ib/II

combination therapy Atezolizumab + Vemurafenib + Cobimetinib

PMIDs:
25037139 27480103 25265494 23934108 22084396 28649441

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB FDA OncoKB
LIFIRAFENIB BRAF

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Details of the Assay for Interaction Inhibition of wild type BRAF kinase domain (aa416-766)

PMIDs:
26208524

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology TTD
PF-04217903 BRAF

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + CGM097 + Dabrafenib + PF-04217903

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
27659046

Sources:
JAX-CKB
PAC-1 BRAF

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27297867

Sources:
JAX-CKB
SELUMETINIB BRAF

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family MEK inhibitor

Alteration BRAF__.

Alteration BRAF:V600E

PMIDs:
24265152 27196754 26351322 23406027 27655129 26137449 22197931 24448821 23942066 26461489 27222538 27312529 19915144 27217440 22048237 26343583 31151904

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC
PD-0325901 BRAF

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
26272063 27488531 26573800 16273091 26267534

Sources:
JAX-CKB
BINIMETINIB BRAF

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Binimetinib

combination therapy Encorafenib + Binimetinib + Cetuximab

Evidence Type Actionable

PMIDs:
26577700 29573941 28152546 23414587 27307593 31566309

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB
XL-888 BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
22351686

Sources:
JAX-CKB
DEL-22379 BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26267534

Sources:
JAX-CKB
ARQ-736 BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
TAK-733 BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Phase I

PMIDs:
26439693 24398428 22798288

Sources:
JAX-CKB
CAPMATINIB BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type collecting duct carcinoma

Response Type sensitive

Approval Status Preclinical - Pdx

PMIDs:
28783719

Sources:
JAX-CKB
DOXIL BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type sensitive

PMIDs:
21216929

Sources:
JAX-CKB
LGX-806 BRAF

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SORAFENIB BRAF

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Nexavar

Novel drug target Established target

Drug family Pan-TK inhibitor

PMIDs:
20812347 16609060 17575107 11752352 16901402 16880785 18794803 19001320 24727320 20526349 18186519 25157968 22310681 20350999 19537845 12068308 20619739 14679157 21129611 26619011 28362716 24885690 23792568 22394203 23629727 27388325 20538618 28002790

Sources:
DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI TEND DoCM CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB
E-6201 BRAF

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
23039341 24448821

Sources:
JAX-CKB
OBATOCLAX BRAF

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
22460902

Sources:
JAX-CKB
GANETESPIB BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type skin melanoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25077897 24398428

Sources:
JAX-CKB
MLN-2480 BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction RAF serine/threonine protein kinase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
IDELALISIB BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical

PMIDs:
26137449

Sources:
JAX-CKB
TIVOZANIB BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy PLX4720 + Tivozanib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
26461489

Sources:
JAX-CKB
AEW-541 BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6482 + NVP-AEW541

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700

Sources:
JAX-CKB
UPROSERTIB BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
24265152

Sources:
JAX-CKB
CGM-097 BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell culture

Indication/Tumor Type colorectal cancer

combination therapy ABT-263 + CGM097 + Dabrafenib + PF-04217903

PMIDs:
27659046

Sources:
JAX-CKB
PIMASERTIB BRAF

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pimasertib + Sorafenib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
23629727

Sources:
ClearityFoundationBiomarkers JAX-CKB
REGORAFENIB BRAF

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
21170960 23629727 25838391

Sources:
DrugBank MyCancerGenome JAX-CKB ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial
NAVITOCLAX BRAF

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy ABT-263 + Alpelisib + Dabrafenib + Erlotinib

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
27659046 24983357 25665005

Sources:
JAX-CKB
SAR-260301 BRAF

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy SAR260301 + Selumetinib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27196754

Sources:
JAX-CKB
REFAMETINIB BRAF

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
19706763

Sources:
JAX-CKB
RO-4987655 BRAF

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26438159

Sources:
JAX-CKB
PF-00477736 BRAF

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell culture

Indication/Tumor Type Advanced Solid Tumor

Indication/Tumor Type colon cancer

PMIDs:
26140595

Sources:
JAX-CKB
DASATINIB BRAF

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect reduced kinase activity

Pathway activation

PMIDs:
20350999 21129611 22310681 25157968 19537845 18186519 26619011 12460919 12460918 21483012 19238210 22649091 12068308 23833300 19010912 23242808 27222538

Sources:
JAX-CKB CGI DoCM MyCancerGenomeClinicalTrial
PERTUZUMAB BRAF

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29320312

Sources:
CIViC
ALPELISIB BRAF

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Alpelisib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27659046 27924459 28363909 26577700 27312529

Sources:
JAX-CKB CGI CIViC
AFATINIB BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26916115

Sources:
JAX-CKB
TEMSIROLIMUS BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Bevacizumab + Temsirolimus + Doxil

Indication/Tumor Type ovarian carcinoma

Response Type sensitive

PMIDs:
21216929

Sources:
JAX-CKB MyCancerGenomeClinicalTrial
EVEROLIMUS BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Everolimus + Selumetinib

Indication/Tumor Type malignant glioma

Response Type predicted – sensitive

PMIDs:
20664172 20664174 23629727 27797976 27217440 29156677

Sources:
JAX-CKB CIViC
IRINOTECAN BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Irinotecan

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
28783719 26989027 22180495 26687137 19603024 27729313 25714871 19603018

Sources:
JAX-CKB CIViC
GSK-2636771 BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GSK2636771 + Pembrolizumab

combination therapy GSK2636771 + unspecified IGF-1R antibody

combination therapy BYL719 + GSK2636771 + LGX818

PMIDs:
26577700 26645196

Sources:
JAX-CKB
NERATINIB BRAF

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
26243863

Sources:
JAX-CKB
PEMBROLIZUMAB BRAF

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical

PMIDs:
26645196

Sources:
JAX-CKB PharmGKB FDA
CI-1040 BRAF

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
19018267 19915144 20538618

Sources:
JAX-CKB
RIPRETINIB BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
AZD-6482 BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6482 + NVP-AEW541

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700

Sources:
JAX-CKB
PA-799 BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type decreased response

Approval Status Preclinical - Cell line xenograft

PMIDs:
21558396

Sources:
JAX-CKB
SARACATINIB BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
23242808

Sources:
JAX-CKB
PEXIDARTINIB BRAF

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy PLX3397 + Vemurafenib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
25939769

Sources:
JAX-CKB
BEVACIZUMAB BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Bevacizumab + Temsirolimus + Doxil

Indication/Tumor Type ovarian carcinoma

Response Type sensitive

PMIDs:
21216929 19603024 22180495 19571295

Sources:
JAX-CKB CIViC
LENVATINIB BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type sensitive

PMIDs:
26169970

Sources:
JAX-CKB
GEDATOLISIB BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
17314276 21325073 24042735

Sources:
JAX-CKB
OXALIPLATIN BRAF

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
26637369 19603024 19571295

Sources:
JAX-CKB CIViC
NIVOLUMAB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
VENETOCLAX BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB
PICTILISIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC0879 + GDC-0941

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
26577700 24265153 19276360

Sources:
JAX-CKB
SAPANISERTIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MLN0128 + PD-0325901

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
26272063 25261369

Sources:
JAX-CKB
RIBOCICLIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Ribociclib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
28351928

Sources:
JAX-CKB
BUPARLISIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + BKM120

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
24265152 27307593

Sources:
JAX-CKB
PANOBINOSTAT BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Lapatinib + Panobinostat

Indication/Tumor Type colorectal cancer

Response Type sensitive

PMIDs:
21464044

Sources:
JAX-CKB
MK-2206 BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MK2206 + Trametinib

Indication/Tumor Type melanoma

PMIDs:
24265152

Sources:
JAX-CKB
ERLOTINIB BRAF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Erlotinib + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27659046 22448344 27924459 22180495

Sources:
JAX-CKB CIViC
LAPATINIB BRAF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type sensitive

combination therapy Lapatinib + Panobinostat

Indication/Tumor Type colorectal cancer

PMIDs:
23365119 21464044

Sources:
JAX-CKB
OMIPALISIB BRAF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dabrafenib + GSK2126458

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
22389471

Sources:
JAX-CKB
PILARALISIB BRAF

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
25637314

Sources:
JAX-CKB
DACTOLISIB BRAF

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Vemurafenib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
23549875 26137449

Sources:
JAX-CKB CIViC
GEFITINIB BRAF

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

combination therapy Gefitinib + PLX4720

Evidence Type Actionable

PMIDs:
27312529 23242808 22448344 22281684

Sources:
JAX-CKB CIViC
TRASTUZUMAB BRAF

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fluorouracil + Leucovorin + Trastuzumab

Indication/Tumor Type rectum adenocarcinoma

Response Type no benefit

PMIDs:
27626067

Sources:
JAX-CKB
CAPECITABINE BRAF

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22180495 19571295

Sources:
CIViC
ATEZOLIZUMAB BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Atezolizumab + Vemurafenib + Cobimetinib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
LEUCOVORIN BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fluorouracil + Leucovorin + Trastuzumab

Indication/Tumor Type rectum adenocarcinoma

Response Type no benefit

PMIDs:
27626067

Sources:
JAX-CKB
PONATINIB BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31937621

Sources:
CIViC
VORUCICLIB BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vemurafenib + Voruciclib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
PALBOCICLIB BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26369631 27488531

Sources:
JAX-CKB
SORAFENIB TOSYLATE BRAF

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CRIZOTINIB BRAF

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Crizotinib;Vemurafenib

Drug family ALK inhibitor;BRAF inhibitor

Alteration MET:amp;BRAF:V600E

PMIDs:
None found

Sources:
CGI
VORINOSTAT BRAF

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

PMIDs:
27924459

Sources:
JAX-CKB
CEDIRANIB BRAF

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type sensitive

combination therapy Cediranib + Selumetinib + PLX4720

Indication/Tumor Type melanoma

PMIDs:
26461489

Sources:
JAX-CKB
IMATINIB BRAF

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

combination therapy Imatinib + PLX4720

Evidence Type Actionable

PMIDs:
27924459

Sources:
JAX-CKB
FLUOROURACIL BRAF

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fluorouracil + Leucovorin + Trastuzumab

Indication/Tumor Type rectum adenocarcinoma

Response Type no benefit

PMIDs:
26637369 27626067

Sources:
JAX-CKB
DOXORUBICIN BRAF

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy PLX4720 + Doxorubicin

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
27924459

Sources:
JAX-CKB
FOSTAMATINIB BRAF

Interaction Score: 0.0

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000157764
- Version: 101_38
Alternate Names:

BRAF Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P15056
- Version: January-2014
Alternate Names:

BRAF Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.11.1

Publications:

RussLampel: ENSG00000157764

Version: 26-July-2011

Alternate Names:

ENSG00000157764 Ensembl Gene Id

BRAF Display Id

B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE (EC 2.7.1.37) (P94) (V-RAF MURINE SARCOMA VIRAL ONCOGENE HOMOLOG B1). [SOURCE:UNIPROT/SWISSPROT;ACC:P15056] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TEND: P15056
- Version: 01-August-2011
Alternate Names:

BRAF1_HUMAN Uniprot Id

ENSG00000157764 Ensembl Gene Id

P15056 Uniprot Accession

Gene Info:

Target Subclass 2.7.11.1

Target Main Class Enzymes

Publications:
CancerCommons: BRAF
- Version: 25-July-2013
Alternate Names:

673 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name BRAF (V660) E/K

CancerCommons Reported Gene Name BRAF

CancerCommons Reported Gene Name Pan-RAF

Publications:
HopkinsGroom: P15056
- Version: 11-September-2012
Alternate Names:

SERINE/THREONINE-PROTEIN KINASE B-RAF Uniprot Protein Name

BRAF_HUMAN Uniprot Id

673 Entrez Gene Id

Gene Info:

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Uniprot Evidence 1: Evidence at protein level

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
GuideToPharmacology: 673
- Version: 29-September-2020
Alternate Names:

1097 HUGO Gene ID

1097 HUGO Gene Symbol

B-Raf proto-oncogene, serine/threonine kinase HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name RAF family

GuideToPharmacology Gene Category ID 610

Gene Categories:

ENZYME

Publications:

JAX-CKB: BRAF

Version: 27-September-2017

Alternate Names:

673 CKB Entrez Id

BRAF CKB Gene Synonym

B-raf CKB Gene Synonym

Gene Info:

Publications:

Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Basile et al., 2014, Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors., Pigment Cell Melanoma Res

PharmGKB: BRAF
- Version: 18-August-2020
Alternate Names:

PA25408 PharmGKB ID

Gene Info:

Publications:

Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics

CIViC: BRAF

Version: 14-September-2020

Alternate Names:

673 Entrez Gene ID

5 CIViC Gene ID

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE, DRUG RESISTANCE

Publications:

Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell

Kocsis J et al., 2017, Combined dabrafenib and trametinib treatment in a case of chemotherapy-refractory extrahepatic BRAF V600E mutant cholangiocarcinoma: dramatic clinical and radiological response with a confusing synchronic new liver lesion., J Gastrointest Oncol

Lavingia V et al., 2016, Impressive response to dual <i>BRAF</i> and MEK inhibition in patients with BRAF mutant intrahepatic cholangiocarcinoma-2 case reports and a brief review., J Gastrointest Oncol

DrugBank: BE0000634

Version: 5.1.7

Alternate Names:

BRAF DrugBank Gene Name

P15056 UniProt Accession

673 Entrez Gene Id

Gene Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

Jordan et al., 2012, Vemurafenib for the treatment of melanoma., Expert Opin Pharmacother

Gibney et al., 2013, Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies., Expert Opin Drug Metab Toxicol

CGI: BRAF

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

De Roock et al., 2010, Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis., Lancet Oncol.

De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.

Peeters et al., 2013, Massively parallel tumor multigene sequencing to evaluate response to panitumumab in a randomized phase III study of metastatic colorectal cancer., Clin. Cancer Res.

DoCM: BRAF

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature

Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol

Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.

DTC: BRAF

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Yang W et al., 2015, Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors., Eur J Med Chem

Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem

HingoraniCasas: ENSG00000157764
- Version: 31-May-2017
Alternate Names:

ENSG00000157764 Gene Symbol

BRAF Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: BRAF
- Version: 12-May-2016
Alternate Names:

BRAF Gene Symbol

Gene Info:

Publications:
MyCancerGenome: BRAF
- Version: 20-Jun-2017
Alternate Names:

673 Entrez Gene Id

BRAF MyCancerGenome Gene Symbol

BRAF MyCancerGenome Reported Gene Name

Gene Info:

Publications:
ChemblInteractions: BRAF1
- Version: chembl_23
Alternate Names:

RAFB1 GENE_SYMBOL

BRAF GENE_SYMBOL

Serine/threonine-protein kinase B-raf UNIPROT

Gene Info:

Publications:
OncoKB: BRAF
- Version: 23-July-2020
Alternate Names:

673 OncoKB Entrez Id

NS7 OncoKB Gene Synonym

B-raf OncoKB Gene Synonym

Gene Info:

Publications:
Pharos: BRAF
- Version: 03-September-2020
Alternate Names:

Serine/threonine-protein kinase B-raf Gene Name

P15056 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: BRAF
- Version: 05-September-2020
Alternate Names:

BRAF1 GO Gene Synonym

RAFB1 GO Gene Synonym

Gene Info:

Gene Categories:

SERINE THREONINE KINASE

Publications:
Tempus: BRAF
- Version: 11-November-2018
Alternate Names:

BRAF Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: BRAF
- Version: 27-Jun-2013
Alternate Names:

673 Gene ID

B-RAF1 dGene Synonym

BRAF1 dGene Synonym

Gene Info:

Gene Categories:

SERINE THREONINE KINASE, KINASE

Publications:
TTD: Serine/threonine-protein kinase B-raf
- Version: 2020.06.01
Alternate Names:

BRAF TTD Gene Abbreviation

T99089 TTD Target ID

Gene Info:

Publications:
ClearityFoundationBiomarkers: BRAF
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
ClearityFoundationClinicalTrial: BRAF
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: BRAF
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
MskImpact: BRAF
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: BRAF
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: BRAF
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: BRAF
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:
Oncomine: BRAF
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
COSMIC: BRAF
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Response Type	predicted – resistant
Indication/Tumor Type	ovarian cancer
combination therapy	AMG 232 + Trametinib + Dabrafenib

Clinical Status	late trials
Clinical Status	early trials
Clinical Status	case report

Alteration	MET:amp;BRAF:V600E
Drug family	BRAF inhibitor;EGFR mAb inhibitor
combination therapy	Vemurafenib;Panitumumab

combination therapy	Trametinib + Dabrafenib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

combination therapy	Cetuximab + Encorafenib
Indication/Tumor Type	colorectal cancer
Response Type	resistant

Indication/Tumor Type	melanoma
Response Type	resistant
Approval Status	Preclinical - Cell line xenograft

combination therapy	Cetuximab + PLX4720
combination therapy	Vemurafenib + Cetuximab
combination therapy	Cetuximab + Dabrafenib + SCH772984

Details of the Assay for Interaction	In a cell-free assay
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

inhibitor (inhibitory)
antagonist (inhibitory)

Mechanism of Interaction	Serine/threonine-protein kinase B-raf inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	Inhibition of wild type BRAF activity.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

combination therapy	Vemurafenib + TW-37
Indication/Tumor Type	non-small cell lung carcinoma
Evidence Type	Actionable

Approval Status	FDA approved
Approval Status	Phase Ib/II
combination therapy	Atezolizumab + Vemurafenib + Cobimetinib

combination therapy	ABT-263 + CGM097 + Dabrafenib + PF-04217903
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

Drug family	MEK inhibitor
Alteration	BRAF__.
Alteration	BRAF:V600E

combination therapy	Encorafenib + Binimetinib
combination therapy	Encorafenib + Binimetinib + Cetuximab
Evidence Type	Actionable

Indication/Tumor Type	collecting duct carcinoma
Response Type	sensitive
Approval Status	Preclinical - Pdx

Trial Name	Nexavar
Novel drug target	Established target
Drug family	Pan-TK inhibitor

Indication/Tumor Type	skin melanoma
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

BRAF Gene Record

BRAF 673 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory) antagonist (inhibitory)

Interaction Info: Response Type predicted – resistant Indication/Tumor Type ovarian cancer combination therapy AMG 232 + Trametinib + Dabrafenib

Sources: TALC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI DoCM COSMIC CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Clinical Status late trials Clinical Status early trials Clinical Status case report

Sources: TALC DTC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Alteration MET:amp;BRAF:V600E Drug family BRAF inhibitor;EGFR mAb inhibitor combination therapy Vemurafenib;Panitumumab

Sources: JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Trametinib + Dabrafenib Indication/Tumor Type colorectal cancer Response Type sensitive

Sources: ClearityFoundationBiomarkers JAX-CKB CGI DoCM CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 23549875

Sources: CIViC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical

PMIDs: 27834212 24422853

Sources: JAX-CKB GuideToPharmacology TTD OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy Cetuximab + Encorafenib Indication/Tumor Type colorectal cancer Response Type resistant

PMIDs: 27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources: TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical - Cell line xenograft

PMIDs: 26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources: DrugBank JAX-CKB CGI CIViC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type predicted – sensitive Response Type resistant

PMIDs: 20538618 22351689

Sources: DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Cetuximab + PLX4720 combination therapy Vemurafenib + Cetuximab combination therapy Cetuximab + Dabrafenib + SCH772984

Sources: JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a cell-free assay Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 27523909 20538618

Sources: JAX-CKB GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of wild type BRAF activity. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 22319199

Sources: JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23398453

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type melanoma Response Type sensitive Approval Status Preclinical

PMIDs: 22798288 26732095 26343583

Sources: JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Vemurafenib + TW-37 Indication/Tumor Type non-small cell lung carcinoma Evidence Type Actionable

PMIDs: 25665005

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Response Type predicted – resistant

Indication/Tumor Type ovarian cancer

combination therapy AMG 232 + Trametinib + Dabrafenib

Sources:
TALC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI DoCM COSMIC CIViC GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status late trials

Clinical Status early trials

Clinical Status case report

Sources:
TALC DTC ClearityFoundationBiomarkers DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration MET:amp;BRAF:V600E

Drug family BRAF inhibitor;EGFR mAb inhibitor

combination therapy Vemurafenib;Panitumumab

Sources:
JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Trametinib + Dabrafenib

Indication/Tumor Type colorectal cancer

Response Type sensitive

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI DoCM CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
23549875

Sources:
CIViC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
27834212 24422853

Sources:
JAX-CKB GuideToPharmacology TTD OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Encorafenib

Indication/Tumor Type colorectal cancer

Response Type resistant

PMIDs:
27307593 28363909 28351928 27312529 26577700 29573941 31566309 29356698 25769717 26586345

Sources:
TALC DrugBank MyCancerGenome JAX-CKB ChemblInteractions CIViC CancerCommons PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources:
DrugBank JAX-CKB CGI CIViC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Response Type resistant

PMIDs:
20538618 22351689

Sources:
DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + PLX4720

combination therapy Vemurafenib + Cetuximab

combination therapy Cetuximab + Dabrafenib + SCH772984

Sources:
JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a cell-free assay

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
27523909 20538618

Sources:
JAX-CKB GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of wild type BRAF activity.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
22319199

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
23398453

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
22798288 26732095 26343583

Sources:
JAX-CKB ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vemurafenib + TW-37

Indication/Tumor Type non-small cell lung carcinoma

Evidence Type Actionable

PMIDs:
25665005

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

PMIDs:
None found

Sources:
CancerCommons

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status FDA approved

Approval Status Phase Ib/II

combination therapy Atezolizumab + Vemurafenib + Cobimetinib

PMIDs:
25037139 27480103 25265494 23934108 22084396 28649441

Mechanism of Interaction	RAF serine/threonine protein kinase inhibitor
Direct Interaction	yes

combination therapy	PLX4720 + Tivozanib
Indication/Tumor Type	melanoma
Response Type	sensitive

combination therapy	AZD6482 + NVP-AEW541
Indication/Tumor Type	melanoma
Response Type	no benefit

Approval Status	Preclinical - Cell culture
Indication/Tumor Type	colorectal cancer
combination therapy	ABT-263 + CGM097 + Dabrafenib + PF-04217903

combination therapy	Pimasertib + Sorafenib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

combination therapy	ABT-263 + Alpelisib + Dabrafenib + Erlotinib
Indication/Tumor Type	colorectal cancer
Response Type	sensitive

combination therapy	SAR260301 + Selumetinib
Indication/Tumor Type	melanoma
Response Type	sensitive

Clinical Status	preclinical
Variant Effect	reduced kinase activity
Pathway	activation

combination therapy	Alpelisib + PLX4720
Indication/Tumor Type	melanoma
Response Type	sensitive

combination therapy	Bevacizumab + Temsirolimus + Doxil
Indication/Tumor Type	ovarian carcinoma
Response Type	sensitive