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Gene | MAP2K1 |
Variant | I111S |
Impact List | missense |
Protein Effect | gain of function |
Gene Variant Descriptions | MAP2K1 I111S lies within the protein kinase domain of the Map2k1 protein (UniProt.org). I111S confers a gain of function on the Map2k1 protein as demonstrated by increased autophosphorylation and Erk phosphorylation and also demonstrates resistance to some Mek and Braf inhibitors (PMID: 29753091). |
Associated Drug Resistance | Y |
Category Variants Paths |
MAP2K1 mutant MAP2K1 act mut MAP2K1 I111S |
Transcript | NM_002755.4 |
gDNA | chr15:g.66436786T>G |
cDNA | c.332T>G |
Protein | p.I111S |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
NM_002755.4 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
NM_002755.3 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
XM_017022411.3 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
NM_002755 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
XM_017022411.2 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
XM_017022411 | chr15:g.66436786T>G | c.332T>G | p.I111S | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
MAP2K1 I111S | Advanced Solid Tumor | resistant | AZD8330 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed resistance to the Mek inhibitor, AZD8330, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 I111S | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 I111S | Advanced Solid Tumor | sensitive | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 I111S | Advanced Solid Tumor | sensitive | PLX4720 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 I111S | Advanced Solid Tumor | resistant | GDC0879 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 I111S | Advanced Solid Tumor | resistant | PD98059 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed resistance to the Mek inhibitor, PD98059, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |