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
Mutation Info Missense: D67N
Mutation Info Missense: E120D
Mutation Info Missense: E203K
Mutation Info Missense: F129L
Mutation Info Missense: F133L
Mutation Info Missense: G128D
Mutation Info Missense: G128V
Mutation Info Missense: H119P
Mutation Info Missense: I103N
Mutation Info Missense: I111N
Mutation Info Missense: I99T
Mutation Info Missense: K104N
Mutation Info Missense: K57E
Mutation Info Missense: K57N
Mutation Info Missense: L115P
Mutation Info Missense: L215P
Mutation Info Missense: P124L
Mutation Info Missense: P124S
Mutation Info Missense: Q56P
Mutation Info Missense: V211D
Mutation Info Missense: V60E
Reference
Ref 555733MEK1 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 555798Dissecting 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 555849ERK 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 555926Phase 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 555935Pharmacodynamic 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 555981The 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 555991BRAF 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.
Ref 556039Increased 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.