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MAP2K1 Gene Record

  • Summary
  • Interactions
  • Claims
  • MAP2K1 5604 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    5604
    MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1
    MAP2K1
    CFC3
    MAPKK1
    MEK1
    MKK1
    PRKMK1
    176872
    6840
    ENSG00000169032
    OTTHUMG00000133196
    Dual specificity mitogen-activated protein kinase kinase 1
    ERK activator kinase 1
    MAPK/ERK kinase 1
    MAP kinase kinase 1
    MAPKK 1
    MEK 1
    BE0000870
    Q02750
    2062
    NM_002755
    NP_002746
    31
    MP2K1_HUMAN
    DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1 (EC 2.7.1.-) (MAP KINASE KINASE 1) (MAPKK 1) (ERK ACTIVATOR KINASE 1) (MAPK/ERK KINASE 1) (MEK1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q02750]
    MEK
    T35940

    Gene Info:

    GuideToPharmacology Gene Category Name STE7 family
    GuideToPharmacology Gene Category ID 623
    Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain
    Interpro Acc IPR002290
    Human Readable Name DRUGGABLE GENOME
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Interpro Short Name Ser/Thr_dual-sp_kinase_dom
    Human Readable Name KINASE
    Uniprot Evidence 1: Evidence at protein level
    CancerCommons Reported Gene Name MEK
    Target Class Enzymes
    Target Subclass EC:2.7.12.2
    Gene Biotype PROTEIN_CODING
    (25 More Sources)

    Gene Categories: Category Details

    KINASE
    SERINE THREONINE KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    NUCLEAR HORMONE RECEPTOR
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE
    ENZYME

    Publications:

    Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
    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.
    Yeh et al., 2007, Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor., Clin. Cancer Res.
    Choi et al., 2012, Oncogenic MAP2K1 mutations in human epithelial tumors., Carcinogenesis
    Crystal et al., 2014, Patient-derived models of acquired resistance can identify effective drug combinations for cancer., Science
    Dombi et al., 2016, Activity of Selumetinib in Neurofibromatosis Type 1-Related Plexiform Neurofibromas., N. Engl. J. Med.
    Marks et al., 2008, Novel MEK1 mutation identified by mutational analysis of epidermal growth factor receptor signaling pathway genes in lung adenocarcinoma., Cancer Res.
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Gannon et al., 2016, Identification of an "Exceptional Responder" Cell Line to MEK1 Inhibition: Clinical Implications for MEK-Targeted Therapy., Mol. Cancer Res.
    Davies et al., 2007, AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models., Mol. Cancer Ther.
    Catalanotti F et al., 2013, Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma., Clin Cancer Res
    Narita et al., 2014, Novel ATP-competitive MEK inhibitor E6201 is effective against vemurafenib-resistant melanoma harboring the MEK1-C121S mutation in a preclinical model., Mol. Cancer Ther.
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Diamond et al., 2016, Diverse and Targetable Kinase Alterations Drive Histiocytic Neoplasms., Cancer Discov
    Singh et al., 2015, Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cells., J. Exp. Clin. Cancer Res.
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
    Bottorff et al., 1995, RAS signalling is abnormal in a c-raf1 MEK1 double mutant., Mol. Cell. Biol.
    Trunzer et al., 2013, Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma., J. Clin. Oncol.
    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.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Carlino et al., 2015, Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients., Clin. Cancer Res.
    Russo et al., 2016, Tumor Heterogeneity and Lesion-Specific Response to Targeted Therapy in Colorectal Cancer., Cancer Discov
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Nelson DS et al., 2015, MAP2K1 and MAP3K1 mutations in Langerhans cell histiocytosis., Genes Chromosomes Cancer
    Brown NA et al., 2014, High prevalence of somatic MAP2K1 mutations in BRAF V600E-negative Langerhans cell histiocytosis., Blood
    Brammeld et al., 2017, Genome-wide chemical mutagenesis screens allow unbiased saturation of the cancer genome and identification of drug resistance mutations., Genome Res.
    Salama et al., 2013, Trametinib (GSK1120212) in the treatment of melanoma., Expert Opin Pharmacother
    Wagle et al., 2014, MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition., Cancer Discov
    Delaney et al., 2002, Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352., Mol. Cell. Biol.
    Gao Y et al., 2019, V211D Mutation in MEK1 Causes Resistance to MEK Inhibitors in Colon Cancer., Cancer Discov
    Remsing Rix et al., 2009, Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells., Leukemia
    Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem
    Daouti S et al., 2010, Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models., Mol Cancer Ther
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
    Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Rizos et al., 2014, BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact., Clin. Cancer Res.
  • CHEMBL485945   MAP2K1

    Interaction Score: 2.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL573819   MAP2K1

    Interaction Score: 2.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • RG-7304   MAP2K1

    Interaction Score: 1.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    25766633


    Sources:
    DTC ChemblInteractions

  • MEKINIST   MAP2K1

    Interaction Score: 1.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    CancerCommons

  • CHEMBL1956073   MAP2K1

    Interaction Score: 1.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20053779


    Sources:
    DTC

  • PIMASERTIB HYDROCHLORIDE   MAP2K1

    Interaction Score: 1.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    CancerCommons

  • COBIMETINIB   MAP2K1

    Interaction Score: 0.98

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Novel drug target Novel Target

    PMIDs:
    26566875 26384788


    Sources:
    ClearityFoundationClinicalTrial CancerCommons MyCancerGenomeClinicalTrial OncoKB JAX-CKB TdgClinicalTrial DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • PD-0325901   MAP2K1

    Interaction Score: 0.96

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    23398453 26267534 25766633 26582713 10592235


    Sources:
    DTC JAX-CKB DrugBank MyCancerGenome ChemblInteractions

  • REFAMETINIB   MAP2K1

    Interaction Score: 0.9

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

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

    PMIDs:
    26582713


    Sources:
    CancerCommons JAX-CKB MyCancerGenome GuideToPharmacology ChemblInteractions

  • RG-7420   MAP2K1

    Interaction Score: 0.79

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes
    Details of the Assay for Interaction Measured in a fluorescence anisotropy assay using recombinant MEK1. Ki approximated from the graph in supplementary figure 1b.

    PMIDs:
    None found


    Sources:
    MyCancerGenome GuideToPharmacology ChemblInteractions

  • SELUMETINIB   MAP2K1

    Interaction Score: 0.75

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

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

    PMIDs:
    22197931 26324360 17332304 22327936 25394791 28029918 18632602 19915144 26582713 17699718 23444215 24448821 27312529


    Sources:
    ClearityFoundationClinicalTrial CancerCommons MyCancerGenomeClinicalTrial JAX-CKB CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • AZD-8330   MAP2K1

    Interaction Score: 0.7

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name AZD-8330
    Novel drug target Novel Target
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • TAK-733   MAP2K1

    Interaction Score: 0.66

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial CancerCommons MyCancerGenome GuideToPharmacology ChemblInteractions

  • E-6201   MAP2K1

    Interaction Score: 0.6

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    24448821


    Sources:
    JAX-CKB GuideToPharmacology ChemblInteractions

  • TRAMETINIB   MAP2K1

    Interaction Score: 0.57

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

    Interaction Info:
    Trial Name GSK1120212
    Novel drug target Novel Target
    Notes

    PMIDs:
    25370473 26644315 24265153 25673644 26566875 26582713 22389471 25899310 27312529 24982505 28179366 23432625 24265154


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial OncoKB JAX-CKB TdgClinicalTrial CIViC DrugBank TALC MyCancerGenome GuideToPharmacology CGI

  • AS-703988   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • COBIMETINIB FUMARATE   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RG-7167   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DEL-22379   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26267534


    Sources:
    JAX-CKB

  • TRAMETINIB DIMETHYL SULFOXIDE   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VEMURAFENIB   MAP2K1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Clinical Status case report
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    22197931 24265153 21383288 7651428 18632602 19915144 23569304 22389471 25157968 24448821 27312529


    Sources:
    DoCM JAX-CKB CIViC CGI

  • PIMASERTIB   MAP2K1

    Interaction Score: 0.47

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial TALC MyCancerGenome ChemblInteractions

  • K-252A   MAP2K1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • DABRAFENIB   MAP2K1

    Interaction Score: 0.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dabrafenib + SCH772984
    Indication/Tumor Type colorectal cancer
    Response Type sensitive

    PMIDs:
    25370473 24265153 25673644 22389471 27312529 24463458 24265154


    Sources:
    JAX-CKB CIViC

  • BINIMETINIB   MAP2K1

    Interaction Score: 0.38

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Negative

    PMIDs:
    31227518


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial TdgClinicalTrial CIViC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ARRY-300   MAP2K1

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name ARRY-300
    Novel drug target Novel Target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • PLX-4720   MAP2K1

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    21383288 19915144


    Sources:
    JAX-CKB

  • RO-4987655   MAP2K1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes
    Reported Cancer Type Melanoma

    PMIDs:
    None found


    Sources:
    CancerCommons ChemblInteractions

  • WX-554   MAP2K1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name WX-554
    Novel drug target Novel Target
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • CI-1040   MAP2K1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

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

    PMIDs:
    12370306 19915144


    Sources:
    JAX-CKB MyCancerGenome GuideToPharmacology ChemblInteractions

  • BALAMAPIMOD   MAP2K1

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PANITUMUMAB   MAP2K1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26644315 31227518


    Sources:
    JAX-CKB CIViC CGI

  • ENCORAFENIB   MAP2K1

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type resistant
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • CERITINIB   MAP2K1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    25394791


    Sources:
    JAX-CKB

  • OMIPALISIB   MAP2K1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type conflicting
    Response Type no benefit
    combination therapy GSK2126458 + Trametinib

    PMIDs:
    22389471


    Sources:
    JAX-CKB

  • CETUXIMAB   MAP2K1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26644315 27312529 28179366


    Sources:
    JAX-CKB CIViC

  • BOSUTINIB   MAP2K1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19039322


    Sources:
    DrugBank

  • ALPELISIB   MAP2K1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    27312529


    Sources:
    JAX-CKB

  • CHEMBL202721   MAP2K1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL406845   MAP2K1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL546797   MAP2K1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL379975   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • JNJ-7706621   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PD-0166285   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • STAUROSPORINE   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • VANDETANIB   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SOTRASTAURIN   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TOZASERTIB   MAP2K1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DOVITINIB   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   MAP2K1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • Ensembl: ENSG00000169032

    • Version: 101_38

    Alternate Names:
    MAP2K1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • HopkinsGroom: Q02750

    • Version: 11-September-2012

    Alternate Names:
    Q02750 Uniprot Accession
    MP2K1_HUMAN Uniprot Id
    5604 Entrez Gene Id

    Gene Info:
    Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain
    Interpro Acc IPR002290
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • RussLampel: ENSG00000169032

    • Version: 26-July-2011

    Alternate Names:
    DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1 (EC 2.7.1.-) (MAP KINASE KINASE 1) (MAPKK 1) (ERK ACTIVATOR KINASE 1) (MAPK/ERK KINASE 1) (MEK1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q02750] Description
    ENSG00000169032 Ensembl Gene Id
    MAP2K1 Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • CancerCommons: MAP2K1

    • Version: 25-July-2013

    Alternate Names:
    5604 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name MEK

    Publications:

  • TdgClinicalTrial: Q02750

    • Version: January-2014

    Alternate Names:
    MAP2K1 Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:2.7.12.2

    Publications:

  • GuideToPharmacology: 5604

    • Version: 29-September-2020

    Alternate Names:
    6840 HUGO Gene ID
    6840 HUGO Gene Symbol
    mitogen-activated protein kinase kinase 1 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name STE7 family
    GuideToPharmacology Gene Category ID 623

    Gene Categories:
    ENZYME

    Publications:

  • JAX-CKB: MAP2K1

    • Version: 27-September-2017

    Alternate Names:
    5604 CKB Entrez Id
    MAP2K1 CKB Gene Synonym
    CFC3 CKB Gene Synonym

    Gene Info:

    Publications:
    Delaney et al., 2002, Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352., Mol. Cell. Biol.
    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.

  • CIViC: MAP2K1

    • Version: 14-September-2020

    Alternate Names:
    5604 Entrez Gene ID
    31 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
    Ahronian et al., 2015, Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations., Cancer Discov
    Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.

  • DrugBank: BE0000870

    • Version: 5.1.7

    Alternate Names:
    MAP2K1 DrugBank Gene Name
    Q02750 UniProt Accession
    5604 Entrez Gene Id

    Gene Info:

    Publications:
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

  • DoCM: MAP2K1

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
    Bottorff et al., 1995, RAS signalling is abnormal in a c-raf1 MEK1 double mutant., Mol. Cell. Biol.
    Marks et al., 2008, Novel MEK1 mutation identified by mutational analysis of epidermal growth factor receptor signaling pathway genes in lung adenocarcinoma., Cancer Res.

  • DTC: MAP2K1

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Van Dort ME et al., 2015, Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor., Bioorg Med Chem
    Daouti S et al., 2010, Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models., Mol Cancer Ther
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem

  • HingoraniCasas: ENSG00000169032

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000169032 Gene Symbol
    MAP2K1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • MyCancerGenome: MAP2K1

    • Version: 20-Jun-2017

    Alternate Names:
    5604 Entrez Gene Id
    MAP2K1 MyCancerGenome Gene Symbol
    MEK MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • TALC: MEK1

    • Version: 12-May-2016

    Alternate Names:
    MEK1 Gene Symbol

    Gene Info:

    Publications:

  • ChemblInteractions: MEK1

    • Version: chembl_23

    Alternate Names:
    PRKMK1 GENE_SYMBOL
    MEK1 GENE_SYMBOL
    MAP2K1 GENE_SYMBOL

    Gene Info:

    Publications:

  • OncoKB: MAP2K1

    • Version: 23-July-2020

    Alternate Names:
    5604 OncoKB Entrez Id
    MKK1 OncoKB Gene Synonym
    PRKMK1 OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: MAP2K1

    • Version: 03-September-2020

    Alternate Names:
    Dual specificity mitogen-activated protein kinase kinase 1 Gene Name
    Q02750 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE, NUCLEAR HORMONE RECEPTOR

    Publications:

  • GO: MAP2K1

    • Version: 05-September-2020

    Alternate Names:
    MEK1 GO Gene Synonym
    PRKMK1 GO Gene Synonym

    Gene Info:

    Gene Categories:
    SERINE THREONINE KINASE, TYROSINE KINASE

    Publications:

  • Tempus: MAP2K1

    • Version: 11-November-2018

    Alternate Names:
    MAP2K1 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: MAP2K1

    • Version: 27-Jun-2013

    Alternate Names:
    5604 Gene ID
    MAPKK1 dGene Synonym
    MEK1 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, SERINE THREONINE KINASE

    Publications:

  • TTD: ERK activator kinase 1

    • Version: 2020.06.01

    Alternate Names:
    MEK1 TTD Gene Abbreviation
    T35940 TTD Target ID

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: MEK1

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: MAP2K1

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CGI: MAP2K1

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: MAP2K1

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • FoundationOneGenes: MAP2K1

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: MAP2K1

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • Oncomine: MAP2K1

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: MAP2K1

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    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