Resistance mutation info of target

Target General Information
Target ID T35940
Target Name Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) Target Info
Gene Name MAP2K1
Species Homo sapiens
Uniprot ID MP2K1_HUMAN
Sequence MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Mutation Info Missense: C121S
Drugs
Drug Name AZD6244 Drug Info [1], [2], [3]
Targeted Disease Cutaneous Melanoma
Mutation Prevalence 16% of the patients
Mutation Info Missense: D67N
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: E120D
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: E203K
Drugs
Drug Name Vemurafenib Drug Info [4]
Targeted Disease Melanoma
Mutation Info Missense: F129L
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name PD0325901 Drug Info [5]
Targeted Disease Cancer
Mutation Info Missense: F133L
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: G128D
Drugs
Drug Name Dabrafenib Drug Info [6]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 10 patients
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: G128V
Drugs
Drug Name Vemurafenib Drug Info [7]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Mutation Info Missense: H119P
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: I103N
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: I111N
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: I99T
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: K104N
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: K57E
Drugs
Drug Name Dabrafenib Drug Info [8]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 30 patients
Drug Name Vemurafenib Drug Info [4]
Targeted Disease Melanoma
Mutation Info Missense: K57N
Drugs
Drug Name AZD6244 Drug Info [1], [2], [3]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: L115P
Drugs
Drug Name PD0325901 Drug Info [5]
Targeted Disease Cancer
Mutation Info Missense: L215P
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: P124L
Drugs
Drug Name Vemurafenib Drug Info [7]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name AZD6244 Drug Info [1], [2], [3]
Targeted Disease Cutaneous Melanoma
Drug Name Selumetinib Drug Info [1]
Targeted Disease Melanoma
Mutation Info Missense: P124S
Drugs
Drug Name Dabrafenib Drug Info [7]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name PLX4720 Drug Info [1], [2]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: Q56P
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name PLX4720 Drug Info [1], [2]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: V211D
Drugs
Drug Name AZD6244 Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Info Missense: V60E
Drugs
Drug Name Vemurafenib Drug Info [7]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Reference
REF 1MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20411-6. doi: 10.1073/pnas.0905833106. Epub 2009 Nov 13.
REF 2Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol. 2011 Aug 1;29(22):3085-96. doi: 10.1200/JCO.2010.33.2312. Epub 2011 Mar 7.
REF 3Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma. Clin Cancer Res. 2013 Apr 15;19(8):2257-64. doi: 10.1158/1078-0432.CCR-12-3476. Epub 2013 Feb 26.
REF 4Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma. J Clin Oncol. 2013 May 10;31(14):1767-74. doi: 10.1200/JCO.2012.44.7888. Epub 2013 Apr 8.
REF 5ERK inhibition overcomes acquired resistance to MEK inhibitors. Mol Cancer Ther. 2012 May;11(5):1143-54. doi: 10.1158/1535-7163.MCT-11-1010. Epub 2012 Mar 8.
REF 6Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma. Nat Commun. 2014 Dec 2;5:5694. doi: 10.1038/ncomms6694.
REF 7The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014 Jan;4(1):94-109. doi: 10.1158/2159-8290.CD-13-0617. Epub 2013 Nov 21.
REF 8BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact. Clin Cancer Res. 2014 Apr 1;20(7):1965-77. doi: 10.1158/1078-0432.CCR-13-3122. Epub 2014 Jan 24.

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