DGIdb - RET Gene Record

RET 5979 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

5979
RET PROTO-ONCOGENE
RET
CDHF12
CDHR16
HSCR1
MEN2A
MEN2B
MTC1
PTC
RET-ELE1
164761
9967
ENSG00000165731
OTTHUMG00000018024
BE0002411
P07949
RET51
RET_HUMAN
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET PRECURSOR (EC 2.7.1.112) (C-RET). [SOURCE:UNIPROT/SWISSPROT;ACC:P07949]
SOLUBLE RET KINASE FRAGMENT
BE0001104
O43519
2185
NP_065681
NM_020630
42
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET
Proto-oncogene c-Ret
Cadherin family member 12
Extracellular cell-membrane anchored RET cadherin 120 kDa fragment
PA34335
T60631

Gene Info:

Target Class	Receptors
Target Subclass	EC:2.7.10.1
Initial Gene Query	RET
Counted Citations from 1950-2000	2777
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Interpro Type	Domain
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
Human Readable Name	KINASE
Interpro Acc	IPR001245
GuideToPharmacology Gene Category Name	Type XIV RTKs: RET
GuideToPharmacology Gene Category ID	794
Target Subclass	Kinase
Target Main Class	Receptors
Target Subclass	Other
Transmembrane Helix Count	1
Gene Biotype	PROTEIN_CODING

(29 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Frisk et al., 2001, CGH alterations in medullary thyroid carcinomas in relation to the RET M918T mutation and clinical outcome., Int. J. Oncol.
Carlomagno et al., 2009, Identification of tyrosine 806 as a molecular determinant of RET kinase sensitivity to ZD6474., Endocr. Relat. Cancer
Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.
Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.
Sherman, 2011, Targeted therapies for thyroid tumors., Mod. Pathol.
Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov
Renaud et al., 1975, Effects of 5,6-dihydroxytryptamine on tyrosine-hydroxylase activity in central catecholaminergic neurons of the rat., Biochem. Pharmacol.
Santoro et al., 1998, Molecular biology of the MEN2 gene., J. Intern. Med.
Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
Couto et al., 2012, AZD1480 blocks growth and tumorigenesis of RET- activated thyroid cancer cell lines., PLoS ONE
Yoh et al., 2017, Vandetanib in patients with previously treated RET-rearranged advanced non-small-cell lung cancer (LURET): an open-label, multicentre phase 2 trial., Lancet Respir Med
Wells et al., 2012, Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial., J. Clin. Oncol.
Wells et al., 2010, Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer., J. Clin. Oncol.
Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.
Lee et al., 2017, Vandetanib in pretreated patients with advanced non-small cell lung cancer-harboring RET rearrangement: a phase II clinical trial., Ann. Oncol.
Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.
Gautschi et al., 2013, A patient with lung adenocarcinoma and RET fusion treated with vandetanib., J Thorac Oncol
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Dabir et al., 2014, RET mutation and expression in small-cell lung cancer., J Thorac Oncol
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Carr et al., 2010, Phase II study of daily sunitinib in FDG-PET-positive, iodine-refractory differentiated thyroid cancer and metastatic medullary carcinoma of the thyroid with functional imaging correlation., Clin. Cancer Res.
Carlomagno et al., 2004, Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors., Oncogene
Vitagliano et al., 2011, The tyrosine kinase inhibitor ZD6474 blocks proliferation of RET mutant medullary thyroid carcinoma cells., Endocr. Relat. Cancer
Gautschi et al., 2017, Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry., J. Clin. Oncol.
Egawa et al., 1998, Genotype-phenotype correlation of patients with multiple endocrine neoplasia type 2 in Japan., Jpn. J. Clin. Oncol.
Elisei et al., 2008, Prognostic significance of somatic RET oncogene mutations in sporadic medullary thyroid cancer: a 10-year follow-up study., J. Clin. Endocrinol. Metab.
Verbeek et al., 2011, The effects of four different tyrosine kinase inhibitors on medullary and papillary thyroid cancer cells., J. Clin. Endocrinol. Metab.
Hatem et al., 2016, Vandetanib as a potential new treatment for estrogen receptor-negative breast cancers., Int. J. Cancer
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
de Groot et al., 2006, Cellular effects of imatinib on medullary thyroid cancer cells harboring multiple endocrine neoplasia Type 2A and 2B associated RET mutations., Surgery
Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
Bentzien et al., 2013, In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer., Thyroid
Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer
Drilon et al., 2016, Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial., Lancet Oncol.
Gild et al., 2013, Targeting mTOR in RET mutant medullary and differentiated thyroid cancer cells., Endocr. Relat. Cancer
Schneider et al., 2015, Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial., Int J Endocrinol
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
Apsel B et al., 2008, Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases., Nat Chem Biol
Plaza-Menacho et al., 2007, Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation independent of proteasomal targeting., J. Biol. Chem.
Wilhelm et al., 2006, Discovery and development of sorafenib: a multikinase inhibitor for treating cancer., Nat Rev Drug Discov
Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
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.
Carlomagno et al., 2006, BAY 43-9006 inhibition of oncogenic RET mutants., J. Natl. Cancer Inst.
Tohyama et al., 2014, Antitumor activity of lenvatinib (e7080): an angiogenesis inhibitor that targets multiple receptor tyrosine kinases in preclinical human thyroid cancer models., J Thyroid Res
Huang et al., 2016, Preclinical Modeling of KIF5B-RET Fusion Lung Adenocarcinoma., Mol. Cancer Ther.
Matsui et al., 2008, E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition., Int. J. Cancer
Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)
Jones et al., 2010, Evolution of an adenocarcinoma in response to selection by targeted kinase inhibitors., Genome Biol.
Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
Kim et al., 2006, An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases., J. Clin. Endocrinol. Metab.
Quintela-Fandino et al., 2014, Selective activity over a constitutively active RET-variant of the oral multikinase inhibitor dovitinib: results of the CNIO-BR002 phase I-trial., Mol Oncol
Mologni et al., 2013, Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase., Mol. Cell. Endocrinol.
De Falco et al., 2013, Ponatinib (AP24534) is a novel potent inhibitor of oncogenic RET mutants associated with thyroid cancer., J. Clin. Endocrinol. Metab.
Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
Lin et al., 2016, Clinical Activity of Alectinib in Advanced RET-Rearranged Non-Small Cell Lung Cancer., J Thorac Oncol
Li et al., 2017, Antitumor Activity of RXDX-105 in Multiple Cancer Types with RET Rearrangements or Mutations., Clin. Cancer Res.
Pietrantonio F et al., 2018, RET fusions in a small subset of advanced colorectal cancers at risk of being neglected., Ann Oncol
Marsee et al., 2004, Inhibition of heat shock protein 90, a novel RET/PTC1-associated protein, increases radioiodide accumulation in thyroid cells., J. Biol. Chem.
Cohen et al., 2002, Inhibition of medullary thyroid carcinoma cell proliferation and RET phosphorylation by tyrosine kinase inhibitors., Surgery
Capes-Davis et al., 1999, Glucocorticoids differentially inhibit expression of the RET proto-oncogene., Gene Expr.
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

CEP-32496 RET

Interaction Score: 1.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
28011461 29538669

Sources:
JAX-CKB CIViC TTD ChemblInteractions
PRALSETINIB RET

Interaction Score: 1.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
OncoKB TTD GuideToPharmacology
CABOZANTINIB RET

Interaction Score: 1.1

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
25366691 8007 23533264 17 21606412 23584301 23705946 28447912 27525386 27825636 2015

Sources:
MyCancerGenomeClinicalTrial OncoKB FDA PharmGKB JAX-CKB CIViC DrugBank TALC MyCancerGenome GuideToPharmacology CGI
CHEMBL306380 RET

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
VANDETANIB RET

Interaction Score: 0.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Direct Interaction? True

PMIDs:
11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

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

Interaction Score: 0.6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
21422803

Sources:
JAX-CKB CIViC TALC MyCancerGenome ChemblInteractions
SUNITINIB RET

Interaction Score: 0.6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
11351254 27149458 20696054 20368568 19255327 18541894 19248971 21455200 16849418 9681850 23056499 22025146 20065189 21422803 25157968 20847059 20943719 28447912 9839497 18073307 21470995

Sources:
NCI TEND PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome GuideToPharmacology CGI
AMUVATINIB RET

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name MP-470

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank TALC MyCancerGenome
ALECTINIB HYDROCHLORIDE RET

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LENVATINIB RET

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
25295214 27496134 17943726

Sources:
JAX-CKB CIViC DrugBank TALC
ALECTINIB RET

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
27544060

Sources:
JAX-CKB CIViC
PONATINIB RET

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
27496134 23811235 25122427 23526464

Sources:
MyCancerGenomeClinicalTrial JAX-CKB CIViC TTD DrugBank TALC GuideToPharmacology
AZD-1480 RET

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
23056499

Sources:
JAX-CKB
REGORAFENIB RET

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
21170960

Sources:
MyCancerGenomeClinicalTrial JAX-CKB TTD DrugBank TALC MyCancerGenome ChemblInteractions
RIVOCERANIB RET

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Assay used apatinib mesylate (YN968D1)

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
QUIZARTINIB RET

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
IMATINIB MESYLATE RET

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12490842

Sources:
NCI
TAFETINIB RET

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a radiometric biochemical protein kinase assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SORAFENIB RET

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
20368568 18849971 17664273 17016424 28362716 15466206 16507829

Sources:
DTC PharmGKB JAX-CKB CIViC DrugBank MyCancerGenome GuideToPharmacology
TANESPIMYCIN RET

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15302866

Sources:
NCI
AST-487 RET

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> inhibition of wild type RET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
23828865

Sources:
DTC CIViC GuideToPharmacology ChemblInteractions
ROMIPLOSTIM RET

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SUNITINIB MALATE RET

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GILTERITINIB RET

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
BARASERTIB RET

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LESTAURTINIB RET

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
SAPANISERTIB RET

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23828865

Sources:
CIViC
LUCITANIB RET

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
ERDAFITINIB RET

Interaction Score: 0.06

Interaction Types & Directionality:

substrate

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
SITRAVATINIB RET

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AT-9283 RET

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
EVEROLIMUS RET

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase II

PMIDs:
26294908 27683183

Sources:
JAX-CKB
SORAFENIB TOSYLATE RET

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CEP-2563 RET

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL202721 RET

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
IMATINIB RET

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name imatinib mesylate, STI 571,Gleevec, Glivec

Novel drug target Established target

PMIDs:
16782438

Sources:
TEND TdgClinicalTrial DrugBank
CEP-11981 RET

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
NINTEDANIB RET

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-TK inhibitor

Alteration RET__.

PMIDs:
None found

Sources:
CGI
AZD-1152-HQPA RET

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB RET

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Phase I

PMIDs:
25103625

Sources:
ClearityFoundationClinicalTrial DTC JAX-CKB
LINIFANIB RET

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name ABT-869, Linifanib

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
DTC TdgClinicalTrial GuideToPharmacology
ENMD-2076 RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ENMD-2076

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
CETUXIMAB RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
LAPATINIB RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SB-220025 RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GENISTEIN RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12490842

Sources:
NCI
CHEMBL546797 RET

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
HESPERADIN RET

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
ALISERTIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1997335 RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SNS-314 RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DEXAMETHASONE RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10947080

Sources:
NCI
OSI-632 RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 RET

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DTC GuideToPharmacology
PAZOPANIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PALBOCICLIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CEDIRANIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
JNJ-7706621 RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PD-0166285 RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB RET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENTRECTINIB RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GW441756X RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
R-406 RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SP-600125 RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB RET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FOSTAMATINIB RET

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000165731
- Version: 101_38
Alternate Names:

RET Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P07949
- Version: 01-August-2011
Alternate Names:

5979 Entrez Gene Id

RET Gene Symbol

ENSG00000165731 Ensembl Gene Id

Gene Info:

Target Subclass Kinase

Target Main Class Receptors

Target Subclass Other

Publications:
TdgClinicalTrial: P07949
- Version: January-2014
Alternate Names:

RET Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:

RussLampel: ENSG00000165731

Version: 26-July-2011

Alternate Names:

PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET PRECURSOR (EC 2.7.1.112) (C-RET). [SOURCE:UNIPROT/SWISSPROT;ACC:P07949] Description

RET Display Id

ENSG00000165731 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

BaderLabGenes: RET
- Version: February-2014
Alternate Names:

5979 Entrez Gene ID

Gene Info:

Initial Gene Query RET

Counted Citations from 1950-2000 2777

Gene Categories:

KINASE

Publications:
HopkinsGroom: P07949
- Version: 11-September-2012
Alternate Names:

RET_HUMAN Uniprot Id

SOLUBLE RET KINASE FRAGMENT Uniprot Protein Name

ENSG00000165731 Ensembl Gene Id

Gene Info:

Uniprot Status Swiss-Prot

Interpro Type Domain

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
GuideToPharmacology: 5979
- Version: 29-September-2020
Alternate Names:

9967 HUGO Gene ID

9967 HUGO Gene Symbol

ret proto-oncogene HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type XIV RTKs: RET

GuideToPharmacology Gene Category ID 794

Publications:

JAX-CKB: RET

Version: 27-September-2017

Alternate Names:

5979 CKB Entrez Id

RET CKB Gene Synonym

CDHF12 CKB Gene Synonym

Gene Info:

Publications:

Schneider et al., 2015, Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial., Int J Endocrinol

Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.

Mologni et al., 2013, Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase., Mol. Cell. Endocrinol.

PharmGKB: RET

Version: 18-August-2020

Alternate Names:

PA34335 PharmGKB ID

Gene Info:

Publications:

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

Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am

Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol

CIViC: RET

Version: 14-September-2020

Alternate Names:

5979 Entrez Gene ID

42 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Couto et al., 2012, AZD1480 blocks growth and tumorigenesis of RET- activated thyroid cancer cell lines., PLoS ONE

Drilon A et al., 2020, Efficacy of Selpercatinib in <i>RET</i> Fusion-Positive Non-Small-Cell Lung Cancer., N Engl J Med

Subbiah V et al., 2018, Selective RET kinase inhibition for patients with RET-altered cancers., Ann Oncol

DrugBank: BE0001104
- Version: 5.1.7
Alternate Names:

RET DrugBank Gene Name

O43519 UniProt Accession

5979 Entrez Gene Id

Gene Info:

Publications:

de Groot et al., 2006, Cellular effects of imatinib on medullary thyroid cancer cells harboring multiple endocrine neoplasia Type 2A and 2B associated RET mutations., Surgery

DrugBank: BE0002411

Version: 5.1.7

Alternate Names:

RET DrugBank Gene Name

P07949 UniProt Accession

5979 Entrez Gene Id

Gene Info:

Publications:

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

Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.

De Falco et al., 2013, Ponatinib (AP24534) is a novel potent inhibitor of oncogenic RET mutants associated with thyroid cancer., J. Clin. Endocrinol. Metab.

NCI: RET

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Cohen et al., 2002, Inhibition of medullary thyroid carcinoma cell proliferation and RET phosphorylation by tyrosine kinase inhibitors., Surgery

Borrello et al., 2005, Induction of a proinflammatory program in normal human thyrocytes by the RET/PTC1 oncogene., Proc. Natl. Acad. Sci. U.S.A.

Bunone et al., 1995, Induction of RET proto-oncogene expression in neuroblastoma cells precedes neuronal differentiation and is not mediated by protein synthesis., Exp. Cell Res.

CGI: RET

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.

Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.

Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov

DoCM: RET

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Frisk et al., 2001, CGH alterations in medullary thyroid carcinomas in relation to the RET M918T mutation and clinical outcome., Int. J. Oncol.

Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.

Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.

DTC: RET

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.

Apsel B et al., 2008, Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases., Nat Chem Biol

TALC: RET
- Version: 12-May-2016
Alternate Names:

RET Gene Symbol

Gene Info:

Publications:
ChemblInteractions: CDHF12
- Version: chembl_23
Alternate Names:

CDHR16 GENE_SYMBOL

PTC GENE_SYMBOL

RET51 GENE_SYMBOL

Gene Info:

Publications:
HingoraniCasas: ENSG00000165731
- Version: 31-May-2017
Alternate Names:

ENSG00000165731 Gene Symbol

RET Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

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

5979 Entrez Gene Id

RET MyCancerGenome Gene Symbol

RET MyCancerGenome Reported Gene Name

Gene Info:

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

5979 OncoKB Entrez Id

MTC1 OncoKB Gene Synonym

CDHF12 OncoKB Gene Synonym

Gene Info:

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

Proto-oncogene tyrosine-protein kinase receptor Ret Gene Name

P07949 UniProt ID

Gene Info:

Gene Categories:

KINASE

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

CDHF12 GO Gene Synonym

CDHR16 GO Gene Synonym

PTC GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE KINASE, DRUG RESISTANCE

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

RET Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

5979 Gene ID

CDHF12 dGene Synonym

CDHR16 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Proto-oncogene c-Ret
- Version: 2020.06.01
Alternate Names:

RET TTD Gene Abbreviation

T60631 TTD Target ID

Gene Info:

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

Gene Info:

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

Gene Info:

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Direct Interaction	yes
Mechanism of Interaction	Tyrosine-protein kinase receptor RET inhibitor
Indication/Tumor Type	non-small cell lung carcinoma

Details of the Assay for Interaction	In a biochemical assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	Zactima
Novel drug target	Established target
Direct Interaction?	True

Evidence Type	Actionable
Approval Status	Preclinical - Cell line xenograft
Response Type	predicted – sensitive

combination therapy	Cetuximab + Sunitinib
Indication/Tumor Type	olfactory neuroblastoma
Response Type	sensitive

Indication/Tumor Type	thyroid medullary carcinoma
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Notes
Mechanism of Interaction	Tyrosine-protein kinase receptor RET inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	Assay used apatinib mesylate (YN968D1)
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	In a radiometric biochemical protein kinase assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	<i>In vitro</i> inhibition of wild type RET.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

antagonist (inhibitory)
inhibitor (inhibitory)

Trial Name	imatinib mesylate, STI 571,Gleevec, Glivec
Novel drug target	Established target

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Phase I

Trial Name	ABT-869, Linifanib
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

5979	Entrez Gene Id
RET	Gene Symbol
ENSG00000165731	Ensembl Gene Id

PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET PRECURSOR (EC 2.7.1.112) (C-RET). [SOURCE:UNIPROT/SWISSPROT;ACC:P07949]	Description
RET	Display Id
ENSG00000165731	Ensembl Gene Id

RET_HUMAN	Uniprot Id
SOLUBLE RET KINASE FRAGMENT	Uniprot Protein Name
ENSG00000165731	Ensembl Gene Id

9967	HUGO Gene ID
9967	HUGO Gene Symbol
ret proto-oncogene	HUGO Gene Name

RET	DrugBank Gene Name
O43519	UniProt Accession
5979	Entrez Gene Id

5979	Entrez Gene Id
RET	MyCancerGenome Gene Symbol
RET	MyCancerGenome Reported Gene Name

5979	OncoKB Entrez Id
MTC1	OncoKB Gene Synonym
CDHF12	OncoKB Gene Synonym

RET Gene Record

RET 5979 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor Indication/Tumor Type non-small cell lung carcinoma

PMIDs: 28011461 29538669

Sources: JAX-CKB CIViC TTD ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a biochemical assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: OncoKB TTD GuideToPharmacology

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

Interaction Info: Details of the Assay for Interaction In a biochemical assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 25366691 8007 23533264 17 21606412 23584301 23705946 28447912 27525386 27825636 2015

Sources: MyCancerGenomeClinicalTrial OncoKB FDA PharmGKB JAX-CKB CIViC DrugBank TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Zactima Novel drug target Established target Direct Interaction? True

PMIDs: 11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell line xenograft Response Type predicted – sensitive

PMIDs: 21422803

Sources: JAX-CKB CIViC TALC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: combination therapy Cetuximab + Sunitinib Indication/Tumor Type olfactory neuroblastoma Response Type sensitive

PMIDs: 11351254 27149458 20696054 20368568 19255327 18541894 19248971 21455200 16849418 9681850 23056499 22025146 20065189 21422803 25157968 20847059 20943719 28447912 9839497 18073307 21470995

Sources: NCI TEND PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Trial Name MP-470 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial DrugBank TALC MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Evidence Type Actionable Approval Status Preclinical Response Type sensitive

PMIDs: 25295214 27496134 17943726

Sources: JAX-CKB CIViC DrugBank TALC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type predicted – sensitive Approval Status Clinical Study

PMIDs: 27544060

Sources: JAX-CKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 27496134 23811235 25122427 23526464

Sources: MyCancerGenomeClinicalTrial JAX-CKB CIViC TTD DrugBank TALC GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type thyroid medullary carcinoma Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 23056499

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor Direct Interaction yes

PMIDs: 21170960

Sources: MyCancerGenomeClinicalTrial JAX-CKB TTD DrugBank TALC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Assay used apatinib mesylate (YN968D1) Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12490842

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a radiometric biochemical protein kinase assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
28011461 29538669

Sources:
JAX-CKB CIViC TTD ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
OncoKB TTD GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
25366691 8007 23533264 17 21606412 23584301 23705946 28447912 27525386 27825636 2015

Sources:
MyCancerGenomeClinicalTrial OncoKB FDA PharmGKB JAX-CKB CIViC DrugBank TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Direct Interaction? True

PMIDs:
11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type predicted – sensitive

PMIDs:
21422803

Sources:
JAX-CKB CIViC TALC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
11351254 27149458 20696054 20368568 19255327 18541894 19248971 21455200 16849418 9681850 23056499 22025146 20065189 21422803 25157968 20847059 20943719 28447912 9839497 18073307 21470995

Sources:
NCI TEND PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name MP-470

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank TALC MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
25295214 27496134 17943726

Sources:
JAX-CKB CIViC DrugBank TALC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
27544060

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
27496134 23811235 25122427 23526464

Sources:
MyCancerGenomeClinicalTrial JAX-CKB CIViC TTD DrugBank TALC GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
23056499

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

PMIDs:
21170960

Sources:
MyCancerGenomeClinicalTrial JAX-CKB TTD DrugBank TALC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Assay used apatinib mesylate (YN968D1)

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
12490842

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a radiometric biochemical protein kinase assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
20368568 18849971 17664273 17016424 28362716 15466206 16507829

Sources:
DTC PharmGKB JAX-CKB CIViC DrugBank MyCancerGenome GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
15302866

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> inhibition of wild type RET.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
23828865

Proto-oncogene tyrosine-protein kinase receptor Ret	Gene Name
P07949	UniProt ID

CDHF12	GO Gene Synonym
CDHR16	GO Gene Synonym
PTC	GO Gene Synonym