Resistance mutation info of drug

Drug General Information
Drug ID D0T5DP
Drug Name AZD6244 Drug Info
Synonyms Selumetinib; ARRY 142886; ARRY142886; AZD 6244; ARRY-142886; ARRY-886; AZD-6244; ARRY-142886, Selumetinib, AZD-6244, ARRY142886, AZD6244
Drug Type Small molecular drug
Company AstraZeneca
Structure D0T5DP
Drug Resistance Mutations
Target Name Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) Target Info
Gene Name MAP2K1
Uniprot ID MP2K1_HUMAN
Species Homo sapiens
Reference Sequence MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV [Homo sapiens]
Targeted Disease Cutaneous Melanoma
Drug Resistance Mutations
Mutation info Missense: C121S [555733], [555798], [555926]
Mutation Prevalence 16% of the patients
Mutation info Missense: P124L [555733], [555798], [555926]
Mutation info Missense: K57N [555733], [555798], [555926]
Mutation info Missense: P124S [555733]
Mutation info Missense: G128D [555733]
Mutation info Missense: F129L [555733]
Mutation info Missense: D67N [555733]
Mutation info Missense: E120D [555733]
Mutation info Missense: F133L [555733]
Mutation info Missense: H119P [555733]
Mutation info Missense: I103N [555733]
Mutation info Missense: I111N [555733]
Mutation info Missense: I99T [555733]
Mutation info Missense: K104N [555733]
Mutation info Missense: L215P [555733]
Mutation info Missense: Q56P [555733]
Mutation info Missense: V211D [555733]
References
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 541008(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5665).
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 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.

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