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BRAF Gene Record

categories for BRAF
  • Summary
  • Interactions
  • Claims
  • 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
    TTDS00346
    B-RAF PROTEIN
    BRAF SERINE/THREONINE KINASE
    BRAF(V599E)
    B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE
    1943
    NP_004324
    NM_004333
    5
    BE0000634
    BRAF1_HUMAN
    BRAF_HUMAN
    RAF

    Gene Info:

    Target Class Enzymes
    Target Subclass EC:2.7.11.1
    Has Variant Annotation false
    Is VIP false
    Human Readable Name DRUGGABLE GENOME
    Gene Biotype PROTEIN_CODING"
    Human Readable Name SERINE THREONINE KINASE
    GuideToPharmacology Gene Category Name RAF family
    GuideToPharmacology Gene Category ID 610
    GuideToPharmacology Gene Type enzyme
    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
    Source Reported Gene Name BRAF
    Gene Category CLINICALLY ACTIONABLE
    (25 More Sources)

    Publications:

    Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov
    Grisham et al., 2015, Extreme Outlier Analysis Identifies Occult Mitogen-Activated Protein Kinase Pathway Mutations in Patients With Low-Grade Serous Ovarian Cancer., J. Clin. Oncol.
    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
    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.
    Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
    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
    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.
    Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
    McNew et al., 2016, MEK and TAK1 Regulate Apoptosis in Colon Cancer Cells with KRAS-Dependent Activation of Proinflammatory Signaling., Mol. Cancer Res.
    Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
    Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
    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.
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
    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.
    James et al., 2012, CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity., Mol. Cancer Ther.
    Su et al., 2012, RAF265 inhibits the growth of advanced human melanoma tumors., Clin. Cancer Res.
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.
    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
    Falchook et al., 2012, Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial., Lancet
    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.
    Fioravanti et al., 1976, Pyridine nucleotide transhydrogenases of parasitic helminths., Arch. Biochem. Biophys.
    Poole-Wilson et al., 1975, Effect of pH on ionic exchange and function in rat and rabbit myocardium., Am. J. Physiol.
    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
    Flaherty et al., 2010, Inhibition of mutated, activated BRAF in metastatic melanoma., N. Engl. J. Med.
    Kim et al., 2013, Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation., Thyroid
    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.
    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
    Gibney et al., 2013, Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies., Expert Opin Drug Metab Toxicol
    Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
    Myall et al., 2016, Long-Term Survival of a Patient With Non-Small-Cell Lung Cancer Harboring a V600E Mutation in the BRAF Oncogene., Clin Lung Cancer
    Schmid et al., 2015, Response to dabrafenib after progression on vemurafenib in a patient with advanced BRAF V600E-mutant bronchial adenocarcinoma., Lung Cancer
    Hyman et al., 2015, Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations., N. Engl. J. Med.
    Peters et al., 2013, Dramatic response induced by vemurafenib in a BRAF V600E-mutated lung adenocarcinoma., J. Clin. Oncol.
    Gautschi et al., 2015, Targeted Therapy for Patients with BRAF-Mutant Lung Cancer: Results from the European EURAF Cohort., J Thorac Oncol
    Robinson et al., 2014, BRAF V600E-mutated lung adenocarcinoma with metastases to the brain responding to treatment with vemurafenib., Lung Cancer
    McGettigan, 2014, Dabrafenib: A New Therapy for Use in BRAF-Mutated Metastatic Melanoma., J Adv Pract Oncol
    Laurent-Puig et al., 2009, Analysis of PTEN, BRAF, and EGFR status in determining benefit from cetuximab therapy in wild-type KRAS metastatic colon cancer., J. Clin. Oncol.
    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.
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.
    Huang et al., 2013, B-Raf and the inhibitors: from bench to bedside., J Hematol Oncol
    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
    Flaherty et al., 2012, Improved survival with MEK inhibition in BRAF-mutated melanoma., 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.
    Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
    Wright et al., 2013, Trametinib: first global approval., Drugs
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
    Johnson et al., 2014, Combined BRAF (Dabrafenib) and MEK inhibition (Trametinib) in patients with BRAFV600-mutant melanoma experiencing progression with single-agent BRAF inhibitor., J. Clin. Oncol.
    Robert et al., 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med.
    Long et al., 2012, Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial., Lancet Oncol.
    Ascierto et al., 2013, Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma., J. Clin. Oncol.
    Long et al., 2014, Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma., N. Engl. J. Med.
    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.
    Flaherty et al., 2012, Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations., N. Engl. J. Med.
    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.
    Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
    Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov
    Ponti et al., 2012, Overwhelming response to Dabrafenib in a patient with double BRAF mutation (V600E; V600M) metastatic malignant melanoma., J Hematol Oncol
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
    Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
    Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
    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.
    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
    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.
    Drobysheva et al., 2017, Targeted MAPK Pathway Inhibitors in Patients With Disseminated Pilocytic Astrocytomas., J Natl Compr Canc Netw
    Agarwal et al., 2016, Response to Targeted Therapy in BRAF Mutant Anaplastic Thyroid Cancer., J Natl Compr Canc Netw
    Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Long GV et al., 2017 Sep 10, Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma., N Engl J Med
    Casadevall et al., 2016, Dabrafenib in an elderly patient with metastatic melanoma and BRAF V600R mutation: a case report., J Med Case Rep
    Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
    2016, Triple Therapy Improves Colorectal Cancer Response., Cancer Discov
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.
    Shen et al., 2016, Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma., Nat. Med.
    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.
    Lu et al., 2017, Engineering and Functional Characterization of Fusion Genes Identifies Novel Oncogenic Drivers of Cancer., Cancer Res.
    Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
    Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
    Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
    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.
    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
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
    Falchook et al., 2012, Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial., Lancet Oncol.
    Kurman et al., 2011, Molecular pathogenesis and extraovarian origin of epithelial ovarian cancer--shifting the paradigm., Hum. Pathol.
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.
    Wan et al., 2004, Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF., Cell
    Howell et al., 2011, Both BRAF V600E mutation and older age (≥ 65 years) are associated with recurrent papillary thyroid cancer., Ann. Surg. 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)
    De Roock et al., 2011, KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer., Lancet Oncol.
    Meckbach et al., 2014, BRAF-V600 mutations have no prognostic impact in stage IV melanoma patients treated with monochemotherapy., PLoS ONE
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    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.
    Zecchin et al., 2013, BRAF V600E is a determinant of sensitivity to proteasome inhibitors., Mol. Cancer Ther.
    Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
    He et al., 2014, Prognostic value of the BRAF V600E mutation in papillary thyroid carcinoma., Oncol Lett
    Patel et al., 2013, Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma., Cancer
    Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
    Morris et al., 2013, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors., Cancer Discov
    Ji et al., 2013, Vemurafenib synergizes with nutlin-3 to deplete survivin and suppresses melanoma viability and tumor growth., Clin. Cancer Res.
    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
    Chapman et al., 2011, Improved survival with vemurafenib in melanoma with BRAF V600E mutation., N. Engl. J. Med.
    Dienstmann et al., 2011, BRAF as a target for cancer therapy., Anticancer Agents Med Chem
    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
    Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov
    Crescenzi et al., 2014, Immunohistochemistry for BRAF(V600E) antibody VE1 performed in core needle biopsy samples identifies mutated papillary thyroid cancers., Horm. Metab. Res.
    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.
    Boulalas et al., Mutational analysis of the BRAF gene in transitional cell carcinoma of the bladder., Int. J. Biol. Markers
    Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
    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
    Jalili et al., 2012, Dual suppression of the cyclin-dependent kinase inhibitors CDKN2C and CDKN1A in human melanoma., J. Natl. Cancer Inst.
    Nissan et al., 2014, Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence., Cancer Res.
    Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
    Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.
    Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
    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.
    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
    Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
    Xing et al., 2014, BRAF V600E and TERT promoter mutations cooperatively identify the most aggressive papillary thyroid cancer with highest recurrence., J. Clin. Oncol.
    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
    Haldar et al., 2011, Epidermal growth factor receptor blockers for the treatment of ovarian cancer., Cochrane Database Syst Rev
    De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
    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.
    Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
    Nagore et al., 2014, Prognostic value of BRAF mutations in localized cutaneous melanoma., J. Am. Acad. Dermatol.
    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.
    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.
    Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
    Chen et al., 2014, BRAFV600E mutation and its association with clinicopathological features of colorectal cancer: a systematic review and meta-analysis., PLoS ONE
    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.
    Lovly et al., 2012, Routine multiplex mutational profiling of melanomas enables enrollment in genotype-driven therapeutic trials., PLoS ONE
    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.
    Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
    Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
    Sosman et al., 2012, Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib., N. Engl. J. Med.
    Tiacci et al., 2011, BRAF mutations in hairy-cell leukemia., N. Engl. J. Med.
    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
    Yang et al., 2012, Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer., Cancer Res.
    Maldonado et al., 2003, Determinants of BRAF mutations in primary melanomas., J. Natl. Cancer Inst.
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    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.
    Nicolaides et al., 2011, Targeted therapy for BRAFV600E malignant astrocytoma., Clin. Cancer Res.
    Dienstmann et al., 2015, Database of genomic biomarkers for cancer drugs and clinical targetability in solid tumors., Cancer Discov
    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.
    Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    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.
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
    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
    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
    Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
    Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
    Basile et al., 2014, Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors., Pigment Cell Melanoma Res
    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
    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.
    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
    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
    Kaul et al., 2012, Pediatric glioma-associated KIAA1549:BRAF expression regulates neuroglial cell growth in a cell type-specific and mTOR-dependent manner., Genes Dev.
    Iyer et al., 2010, Sorafenib: a clinical and pharmacologic review., Expert Opin Pharmacother
    Kwitkowski et al., 2010, FDA approval summary: temsirolimus as treatment for advanced renal cell carcinoma., Oncologist
    White et al., 2015, The discovery and development of sorafenib for the treatment of thyroid cancer., Expert Opin Drug Discov
    Wilhelm et al., 2004, BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis., Cancer Res.
    Subbiah et al., 2014, Targeted therapy by combined inhibition of the RAF and mTOR kinases in malignant spindle cell neoplasm harboring the KIAA1549-BRAF fusion protein., J Hematol Oncol
    Palanisamy et al., 2010, Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma., Nat. Med.
    Nakaoku et al., 2014, Druggable oncogene fusions in invasive mucinous lung adenocarcinoma., Clin. Cancer Res.
    Eisen et al., 2006, Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis., Br. J. Cancer
    Haluska et al., 2006, Therapeutic targets in melanoma: map kinase pathway., Curr Oncol Rep
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Kim et al., 2007, Sorafenib inhibits the angiogenesis and growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice., Mol. Cancer Ther.
    Flaherty, 2006, Chemotherapy and targeted therapy combinations in advanced melanoma., Clin. Cancer Res.
    Lu et al., 2010, Sorafenib induces growth inhibition and apoptosis of human chondrosarcoma cells by blocking the RAF/ERK/MEK pathway., J Surg Oncol
    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
    Mangana et al., 2012, Sorafenib in melanoma., Expert Opin Investig Drugs
    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.
    Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
    Smalley et al., 2009, CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations., Oncogene
    Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
    Dietrich et al., 2012, BRAF inhibition in refractory hairy-cell leukemia., N. Engl. J. Med.
    Whittaker et al., 2013, A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition., Cancer Discov
    Savarese et al., beta-Adrenergic receptor decrease in diabetic rat hearts., Life Sci.
    Jordan et al., 2012, Vemurafenib for the treatment of melanoma., Expert Opin Pharmacother
    Ali et al., 2014, Extended Antitumor Response of a BRAF V600E Papillary Thyroid Carcinoma to Vemurafenib., Case Rep Oncol
    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.
    Sharman et al., 2014, Vemurafenib response in 2 patients with posttransplant refractory BRAF V600E-mutated multiple myeloma., Clin Lymphoma Myeloma Leuk
    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
    Hutchinson et al., 2013, BRAF fusions define a distinct molecular subset of melanomas with potential sensitivity to MEK inhibition., Clin. Cancer Res.
    Bahadoran et al., 2013, Major clinical response to a BRAF inhibitor in a patient with a BRAF L597R-mutated melanoma., J. Clin. Oncol.
    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
    Wagenaar et al., 2014, Resistance to vemurafenib resulting from a novel mutation in the BRAFV600E kinase domain., Pigment Cell Melanoma Res
    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
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Choi et al., 2014, Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors., Pigment Cell Melanoma Res
    Yao et al., 2015, BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition., Cancer Cell
    Nazarian et al., 2010, Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation., Nature
    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.
    Peh et al., 2016, The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas., Mol. Cancer Ther.
    Yaeger et al., 2015, Pilot trial of combined BRAF and EGFR inhibition in BRAF-mutant metastatic colorectal cancer patients., Clin. 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
    Kirouac et al., 2017, Clinical responses to ERK inhibition in BRAF(V600E)-mutant colorectal cancer predicted using a computational model., NPJ Syst Biol Appl
    Banerjee et al., 2016, A Rare Finding of a BRAF Mutation in Renal Cell Carcinoma with Response to BRAF-Directed Targeted Therapy., Cureus
    Kopetz et al., 2015, Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer., J. Clin. Oncol.
    Feng et al., 2015, SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex., Cancer Res.
    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.
    Connolly et al., 2014, Anticancer activity of combination targeted therapy using cetuximab plus vemurafenib for refractory BRAF (V600E)-mutant metastatic colorectal carcinoma., Curr Oncol
    Mok et al., 2015, Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition., BMC Cancer
    Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., 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)
    Gautschi et al., 2013, Lung adenocarcinoma with BRAF G469L mutation refractory to vemurafenib., Lung Cancer
    Joshi et al., 2015, Trametinib with or without vemurafenib in BRAF mutated non-small cell lung cancer., PLoS ONE
    Kordes et al., 2016, Cooperation of BRAF(F595L) and mutant HRAS in histiocytic sarcoma provides new insights into oncogenic BRAF signaling., Leukemia
    Kotschy et al., 2016, The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models., Nature
    Budina-Kolomets et al., 2016, HSP70 Inhibition Limits FAK-Dependent Invasion and Enhances the Response to Melanoma Treatment with BRAF Inhibitors., Cancer Res.
    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.
    Jing et al., 2012, Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212., Mol. Cancer Ther.
    Bowyer et al., 2014, Activity of trametinib in K601E and L597Q BRAF mutation-positive metastatic melanoma., Melanoma Res.
    Ross et al., 2016, The distribution of BRAF gene fusions in solid tumors and response to targeted therapy., Int. J. Cancer
    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.
    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.
    Lange et al., 2014, Biological and molecular effects of small molecule kinase inhibitors on low-passage human colorectal cancer cell lines., Biomed Res Int
    Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE
    Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.
    Marconcini et al., 2017, Metastatic BRAF K601E-mutated melanoma reaches complete response to MEK inhibitor trametinib administered for over 36 months., Exp Hematol Oncol
    Manchado et al., 2016, A combinatorial strategy for treating KRAS-mutant lung cancer., Nature
    Heidorn et al., 2010, Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF., Cell
    Müller-Gärtner et al., 1989, [Long-term results following surgery or radioiodine treatment of solitary autonomous adenoma of the thyroid gland]., Chirurg
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., 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
    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.
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    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.
    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.
    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.
    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.
    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
    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.
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
    Solit et al., 2006, BRAF mutation predicts sensitivity to MEK inhibition., Nature
    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.
    Acquaviva et al., 2014, Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib., 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
    Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov
    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.
    Mohseni et al., 2010, PIK3CA and KRAS mutations predict for response to everolimus therapy: now that's RAD001., J. Clin. Invest.
    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.
    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
    Herath et al., 2016, The DNA Repair Inhibitor DT01 as a Novel Therapeutic Strategy for Chemosensitization of Colorectal Liver Metastasis., Mol. Cancer Ther.
    Dietlein et al., 2015, A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer., Cell
    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.
    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
    Byron et al., 2012, Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status., Mol. Cancer
    Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
    Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
    Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. 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.
    Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
    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.
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
    Otani et al., 2015, TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer Cells., PLoS ONE
    Garnett et al., 2012, Systematic identification of genomic markers of drug sensitivity in cancer cells., Nature
    Woan et al., 2015, Targeting histone deacetylase 6 mediates a dual anti-melanoma effect: Enhanced antitumor immunity and impaired cell proliferation., Mol Oncol
    Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.
  • BGB-283   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Details of the Assay for Interaction Inhibition of wild type BRAF kinase domain (aa416-766)
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    Publications:
    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.

  • CEP-32496   BRAF

    Interaction Types:
    inhibitor

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

    Publications:
    James et al., 2012, CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity., Mol. Cancer Ther.

  • CHIR-265   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Trial Name CHIR-265
    Novel drug target Established target
    Specific Action of the Ligand Inhibition

    Publications:
    Su et al., 2012, RAF265 inhibits the growth of advanced human melanoma tumors., Clin. Cancer Res.
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med

  • CHEMBL525191   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type resistant
    Approval Status Preclinical - Pdx

    Publications:
    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.
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. Cancer Res.

  • LY-3009120   BRAF

    Interaction Types:
    inhibitor

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

    Publications:
    Chen et al., 2016, Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120., Cancer Discov
    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
    Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov

  • PLX-4720   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Drug family BRAF inhibitor
    Alteration BRAF:V600E
    Specific Action of the Ligand Inhibition

    Publications:
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    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.

  • PLX-8394   BRAF

    Interaction Types:
    inhibitor

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

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

  • REGORAFENIB   BRAF

    Interaction Types:
    inhibitor

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

    Publications:
    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.
    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
    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

  • SB590885   BRAF

    Interaction Types:
    inhibitor

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

    Publications:
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell

  • ENCORAFENIB   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Notes
    combination therapy LGX818 + Cetuximab + BYL719
    Indication/Tumor Type colorectal cancer

    Publications:
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., 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

  • DASATINIB   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Drug family BCR-ABL inhibitor 2nd gen
    Alteration BRAF:Y472C
    Alteration BRAF:G466V

    Publications:
    Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
    Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
    Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature

  • CHEMBL373011   BRAF

    Interaction Types:
    inhibitor

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

    Publications:

  • XL-281   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Trial Name XL281
    Novel drug target Established target
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor

    Publications:

  • ARQ-736   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Mechanism of Interaction Serine/threonine-protein kinase B-raf inhibitor
    Direct Interaction yes
    Notes Targets wildtype BRAF and BRAF with V600E mutation

    Publications:

  • RG-7256   BRAF

    Interaction Types:
    inhibitor

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

    Publications:

  • CHEMBL523411   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Trial Name GSK2118436
    Novel drug target Established target

    Publications:

  • DABRAFENIB MESYLATE   BRAF

    Interaction Types:
    inhibitor

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

    Publications:

  • MLN-2480   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Mechanism of Interaction RAF serine/threonine protein kinase inhibitor
    Direct Interaction yes
    Indication/Tumor Type Advanced Solid Tumor

    Publications:

  • SORAFENIB TOSYLATE   BRAF

    Interaction Types:
    inhibitor

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

    Publications:

  • LGX-806   BRAF

    Interaction Types:
    inhibitor

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

    Publications:

  • DABRAFENIB   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    combination therapy Dabrafenib;Trametinib
    Drug family BRAF inhibitor;MEK inhibitor
    Alteration BRAF:V600E

    Publications:
    Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.

  • SORAFENIB   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    combination therapy Sorafenib + Temsirolimus
    Trial Name Nexavar
    Novel drug target Established target

    Publications:
    Kaul et al., 2012, Pediatric glioma-associated KIAA1549:BRAF expression regulates neuroglial cell growth in a cell type-specific and mTOR-dependent manner., Genes Dev.
    Iyer et al., 2010, Sorafenib: a clinical and pharmacologic review., Expert Opin Pharmacother
    Kwitkowski et al., 2010, FDA approval summary: temsirolimus as treatment for advanced renal cell carcinoma., Oncologist

  • VEMURAFENIB   BRAF

    Interaction Types:
    inhibitor

    Interaction Info:
    Trial Name PLX4032, RG7204
    Novel drug target Established target
    Drug family BRAF inhibitor

    Publications:
    Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
    Dietrich et al., 2012, BRAF inhibition in refractory hairy-cell leukemia., N. Engl. J. Med.
    Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov

  • TEMSIROLIMUS   BRAF

    Interaction Types:
    inhibitor

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

    Publications:
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
    Kaul et al., 2012, Pediatric glioma-associated KIAA1549:BRAF expression regulates neuroglial cell growth in a cell type-specific and mTOR-dependent manner., Genes Dev.
    Iyer et al., 2010, Sorafenib: a clinical and pharmacologic review., Expert Opin Pharmacother

  • PEMBROLIZUMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical

    Publications:
    Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov

  • SELUMETINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Selumetinib + Paclitaxel
    Drug family MEK inhibitor
    Alteration BRAF__.

    Publications:
    Grisham et al., 2015, Extreme Outlier Analysis Identifies Occult Mitogen-Activated Protein Kinase Pathway Mutations in Patients With Low-Grade Serous Ovarian Cancer., J. Clin. Oncol.
    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
    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.

  • BINIMETINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Encorafenib + Binimetinib + Cetuximab
    combination therapy Binimetinib + BKM120
    Indication/Tumor Type melanoma

    Publications:
    Laurent-Puig et al., 2009, Analysis of PTEN, BRAF, and EGFR status in determining benefit from cetuximab therapy in wild-type KRAS metastatic colon cancer., J. Clin. Oncol.
    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.
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.

  • PD-0325901   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type resistant
    Approval Status Preclinical

    Publications:
    Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
    Solit et al., 2006, BRAF mutation predicts sensitivity to MEK inhibition., Nature
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.

  • PIMASERTIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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

  • ALPELISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Panitumumab;Dabrafenib;BYL719
    Drug family EGFR mAb inhibitor;BRAF inhibitor;PI3K inhibitor
    Alteration BRAF:V600.

    Publications:
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., 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
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

  • PICTILISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy GDC0879 + GDC-0941
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
    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.
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov

  • GEFITINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + Gefitinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    Publications:
    Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
    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
    Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov

  • DACTOLISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Coffee et al., 2013, Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer., Clin. 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

  • IRINOTECAN   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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
    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.
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature

  • TAK-733   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov
    Acquaviva et al., 2014, Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib., 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

  • NERATINIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Kavuri et al., 2015, HER2 activating mutations are targets for colorectal cancer treatment., Cancer Discov

  • LENVATINIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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.

  • BUPARLISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Binimetinib + BKM120
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov

  • PALBOCICLIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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.
    Ziemke et al., 2016, Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6., Clin. Cancer Res.

  • EVEROLIMUS   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Everolimus + Selumetinib
    Indication/Tumor Type malignant glioma
    Response Type predicted – sensitive

    Publications:
    Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
    Gibson et al., 2017, Genomic Heterogeneity and Exceptional Response to Dual Pathway Inhibition in Anaplastic Thyroid Cancer., Clin. Cancer Res.
    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

  • IMATINIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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

  • FLUOROURACIL   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    Publications:
    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
    Herath et al., 2016, The DNA Repair Inhibitor DT01 as a Novel Therapeutic Strategy for Chemosensitization of Colorectal Liver Metastasis., Mol. Cancer Ther.

  • LEUCOVORIN   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    Publications:
    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

  • TRASTUZUMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Fluorouracil + Leucovorin + Trastuzumab
    Indication/Tumor Type rectum adenocarcinoma
    Response Type no benefit

    Publications:
    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

  • CHEMBL1231206   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy PF3644022 + PF-477736
    Indication/Tumor Type lung adenocarcinoma
    Response Type predicted – sensitive

    Publications:
    Dietlein et al., 2015, A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer., Cell

  • PF-00477736   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy PF3644022 + PF-477736
    Indication/Tumor Type lung adenocarcinoma
    Response Type predicted – sensitive

    Publications:
    Dietlein et al., 2015, A Synergistic Interaction between Chk1- and MK2 Inhibitors in KRAS-Mutant Cancer., Cell

  • CI-1040   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer

  • CHEMBL2204502   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Paraiso et al., 2012, The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms., Clin. Cancer Res.

  • LAPATINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Lapatinib + Panobinostat
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    Publications:
    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.
    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

  • PANOBINOSTAT   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Lapatinib + Panobinostat
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    Publications:
    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.

  • GANETESPIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Acquaviva et al., 2014, Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib., 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

  • TIVOZANIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE

  • CHEMBL217354   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Trametinib + TW-37
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Lin et al., 2015, The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies., Nat. Genet.

  • DOXORUBICIN   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy PLX4720 + Doxorubicin
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    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

  • BI-2536   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type glioblastoma multiforme
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    Publications:
    Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.

  • OMIPALISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + GSK2126458
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    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.

  • E-6201   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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.
    Byron et al., 2012, Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status., Mol. Cancer

  • NAVITOCLAX   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Trametinib + Navitoclax
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    Publications:
    Lin et al., 2015, The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies., Nat. Genet.
    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
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

  • CEDIRANIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Cediranib + Selumetinib + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE

  • GEDATOLISIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Ahmed et al., 2013, Epigenetic and genetic features of 24 colon cancer cell lines., Oncogenesis
    Mallon et al., 2011, Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor., Clin. Cancer Res.
    Hollestelle et al., 2007, Phosphatidylinositol-3-OH kinase or RAS pathway mutations in human breast cancer cell lines., Mol. Cancer Res.

  • SARACATINIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov

  • Ribociclib   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Encorafenib + Ribociclib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    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.

  • ERLOTINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Erlotinib + PLX4720
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    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
    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
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

  • AFATINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy BI 882370 + Afatinib
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    Publications:
    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.

  • Ro-4987655   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.

  • Refametinib   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Iverson et al., 2009, RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer., Cancer Res.

  • VORINOSTAT   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy PLX4720 + Vorinostat
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    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

  • OXALIPLATIN   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy DT01 + Fluorouracil + Oxaliplatin
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    Publications:
    Herath et al., 2016, The DNA Repair Inhibitor DT01 as a Novel Therapeutic Strategy for Chemosensitization of Colorectal Liver Metastasis., Mol. Cancer Ther.

  • ARQ-092   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy ARQ092 + Trametinib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Yu et al., 2015, Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092., PLoS ONE

  • INK-128   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Hassan et al., 2014, Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors., Oncotarget
    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.

  • PLX-3397   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy PLX3397 + Vemurafenib
    Indication/Tumor Type melanoma
    Response Type sensitive

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

  • PILARALISIB (CHEMBL3218575)   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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.

  • GSK-2636771   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy GSK2636771 + unspecified PD-1 antibody
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

  • PHENMETRAZINE   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical

    Publications:
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol

  • ZSTK-474   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + ZSTK474
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol

  • IDELALISIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type no benefit
    Approval Status Preclinical

    Publications:
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol

  • VENETOCLAX   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Venetoclax + VX-11e
    Indication/Tumor Type colorectal cancer
    Response Type no benefit

    Publications:
    Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med

  • CHEMBL458997   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive
    Approval Status Preclinical

    Publications:
    Otani et al., 2015, TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer Cells., PLoS ONE

  • CAPMATINIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature

  • AZD-6482   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

  • AEW-541   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

  • OBATOCLAX   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Garnett et al., 2012, Systematic identification of genomic markers of drug sensitivity in cancer cells., Nature

  • TUBASTATIN A   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Woan et al., 2015, Targeting histone deacetylase 6 mediates a dual anti-melanoma effect: Enhanced antitumor immunity and impaired cell proliferation., Mol Oncol

  • LY-294002   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy E6201 + LY294002
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Byron et al., 2012, Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status., Mol. Cancer

  • PF-04217903   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Horn et al., 2016, High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells., Cancer Res.

  • SAR-260301   BRAF

    Interaction Types:
    n/a

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

    Publications:
    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.

  • UPROSERTIB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov

  • MK-2206   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy MK2206 + Trametinib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov

  • BEVACIZUMAB   BRAF

    Interaction Types:
    n/a

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

    Publications:
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.

  • PA-799   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type decreased response
    Approval Status Preclinical - Cell line xenograft

    Publications:
    Tanaka et al., 2011, The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations., Clin. Cancer Res.

  • CRIZOTINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Crizotinib;Vemurafenib
    Drug family ALK inhibitor;BRAF inhibitor
    Alteration MET:amp;BRAF:V600E

    Publications:

  • Voruciclib   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Vemurafenib + Voruciclib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:

  • ATEZOLIZUMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Atezolizumab + Vemurafenib + Cobimetinib
    Indication/Tumor Type melanoma
    Response Type sensitive

    Publications:

  • CHEMBL526479   BRAF

    Interaction Types:
    n/a

    Interaction Info:

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

  • TRAMETINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Dabrafenib;Trametinib
    Drug family BRAF inhibitor;MEK inhibitor
    Alteration BRAF:V600E

    Publications:
    Corcoran et al., 2015, Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600-Mutant Colorectal Cancer., J. Clin. Oncol.
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    Sakaguchi et al., 1976, Microbiological oxidation of synthetic chalcocite and covellite by Thiobacillus ferrooxidans., Appl. Environ. Microbiol.

  • PANITUMUMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Panitumumab;Dabrafenib;BYL719
    Drug family EGFR mAb inhibitor;BRAF inhibitor;PI3K inhibitor
    Alteration BRAF:V600.

    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.

  • CETUXIMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    Drug family EGFR mAb inhibitor
    Alteration BRAF:V600E
    combination therapy Dabrafenib + Cetuximab

    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.

  • COBIMETINIB   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Vemurafenib;Cobimetinib
    Drug family BRAF inhibitor;MEK inhibitor
    Alteration BRAF:V600E,V600K

    Publications:
    Hauschild et al., 2012, Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial., Lancet
    Wright et al., 2013, Trametinib: first global approval., Drugs
    Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.

  • PACLITAXEL   BRAF

    Interaction Types:
    n/a

    Interaction Info:
    combination therapy Selumetinib + Paclitaxel

    Publications:
    Grisham et al., 2015, Extreme Outlier Analysis Identifies Occult Mitogen-Activated Protein Kinase Pathway Mutations in Patients With Low-Grade Serous Ovarian Cancer., J. Clin. Oncol.

  • NIVOLUMAB   BRAF

    Interaction Types:
    n/a

    Interaction Info:

    Publications:

  • Ensembl: ENSG00000157764

    • Version: 90_38

    Alternate Names:
    BRAF Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING"

    Publications:

  • dGene: 673

    • Version: 27-June-2013

    Alternate Names:
    673 Entrez Gene Id
    BRAF Gene Symbol

    Gene Info:
    Human Readable Name SERINE THREONINE KINASE

    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:
    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
    BRAF Display Id
    ENSG00000157764 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Publications:

  • TEND: P15056

    • Version: 01-August-2011

    Alternate Names:
    673 Entrez Gene Id
    BRAF Gene Symbol
    P15056 Uniprot Accession

    Gene Info:
    Target Subclass 2.7.11.1
    Target Main Class Enzymes

    Publications:

  • FoundationOneGenes: BRAF

    • Version: 20-September-2013

    Alternate Names:
    673 Entrez Gene ID

    Gene Info:
    Source Reported Gene Name BRAF
    Gene Category CLINICALLY ACTIONABLE

    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:
    BRAF Uniprot Gene Name
    P15056 Uniprot Accession
    ENSG00000157764 Ensembl 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

    Publications:

  • GuideToPharmacologyGenes: 1943

    • Version: 4-March-2015

    Alternate Names:
    673 Entrez Gene ID
    P15056 SwissProt Accession
    NP_004324 RefSeq Protein Accession

    Gene Info:
    GuideToPharmacology Gene Category Name RAF family
    GuideToPharmacology Gene Category ID 610
    GuideToPharmacology Gene Type enzyme

    Publications:

  • PharmGKB: PA25408

    • Version: 12-July-2012

    Alternate Names:
    v-raf murine sarcoma viral oncogene homolog B1 Gene Name
    ENSG00000157764 Ensembl Gene Id
    673 Entrez Gene Id

    Gene Info:
    Has Variant Annotation false
    Is VIP false

    Publications:

  • OncoKB: BRAF

    • Version: 27-September-2017

    Alternate Names:
    B-RAF1 OncoKB Gene Synonym
    RAFB1 OncoKB Gene Synonym
    BRAF1 OncoKB Gene Synonym

    Gene Info:

    Publications:
    Laurent-Puig et al., 2009, Analysis of PTEN, BRAF, and EGFR status in determining benefit from cetuximab therapy in wild-type KRAS metastatic colon cancer., J. Clin. Oncol.
    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.
    Di Nicolantonio et al., 2008, Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer., J. Clin. Oncol.

  • CIViC: BRAF

    • Version: 27-September-2017

    Alternate Names:
    5 CIViC Gene ID
    673 Entrez Gene ID

    Gene Info:

    Publications:
    Menzies et al., 2014, Dabrafenib and trametinib, alone and in combination for BRAF-mutant metastatic melanoma., Clin. Cancer Res.
    Robert et al., 2015, Improved overall survival in melanoma with combined dabrafenib and trametinib., N. Engl. J. Med.
    Klempner et al., 2016, BRAFV600E Mutations in High-Grade Colorectal Neuroendocrine Tumors May Predict Responsiveness to BRAF-MEK Combination Therapy., Cancer Discov

  • CKB: BRAF

    • Version: 27-September-2017

    Alternate Names:
    RAFB1 CKB Gene Synonym
    NS7 CKB Gene Synonym
    BRAF1 CKB Gene Synonym

    Gene Info:

    Publications:
    Yao et al., 2017, Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS., Nature
    Dahlman et al., 2012, BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors., Cancer Discov

  • DrugBank: BE0000634

    • Version: 5.0.8

    Alternate Names:
    ENSG00000157764 Ensembl Gene Id
    673 Entrez Gene Id
    P15056 UniProt Accession

    Gene Info:

    Publications:
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Eisen et al., 2006, Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis., Br. J. Cancer
    Haluska et al., 2006, Therapeutic targets in melanoma: map kinase pathway., Curr Oncol Rep

  • CGI: BRAF

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Gautschi et al., 2012, A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib., J Thorac Oncol
    Dietrich et al., 2012, BRAF inhibition in refractory hairy-cell leukemia., N. Engl. J. Med.
    Andrulis et al., 2013, Targeting the BRAF V600E mutation in multiple myeloma., Cancer Discov

  • 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.

  • GuideToPharmacologyInteractions: 1943

    • Version: 27-September-2017

    Alternate Names:
    P15056 UniProtKB ID
    B-Raf proto-oncogene, serine/threonine kinase GuideToPharmacology Name

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000157764

    • Version: 31-May-2017

    Alternate Names:
    BRAF Ensembl Id
    ENSG00000157764 Gene Symbol

    Gene Info:

    Publications:

  • TALC: BRAF

    • Version: 12-May-2016

    Alternate Names:
    BRAF Gene Symbol

    Gene Info:

    Publications:

  • GO: BRAF

    • Version: 27-September-2017

    Alternate Names:
    RAFB1 GO Gene Synonym
    BRAF1 GO Gene Synonym
    BRAF_HUMAN GO Gene Synonym

    Gene Info:

    Publications:

  • TTD: TTDS00346

    • Version: 4.3.02 (25-August-2011)

    Alternate Names:
    v-raf murine sarcoma viral oncogene homolog B1 Gene Synonym
    ENSG00000157764 Ensembl Gene Id
    673 Entrez Gene Id

    Gene Info:

    Publications:

  • MyCancerGenome: BRAF

    • Version: 20-Jun-2017

    Alternate Names:
    RAF MyCancerGenome Reported Gene Name
    BRAF MyCancerGenome Reported Gene Name
    BRAF MyCancerGenome Gene Symbol

    Gene Info:

    Publications:

  • ChemblInteractions: BRAF1

    • Version: chembl_23

    Alternate Names:
    BRAF1 GENE_SYMBOL
    v-Raf murine sarcoma viral oncogene homolog B1 UNIPROT
    p94 UNIPROT

    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:

  • CarisMolecularIntelligence: BRAF

    • Version: 07-October-2015

    Alternate Names:

    Gene Info:

    Publications:

  • FDA: BRAF

    • Version: 15-September-2017

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: BRAF

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v3.0.2 - sha1 ec916b2) • Last updated 2018-01-25