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RET Gene Record

  • Summary
  • Interactions
  • Claims
  • 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:

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 (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21