Resistance mutation info of target

Target General Information
Target ID T09826
Target Name Toposisomerase-1 (TOP1) Target Info
Gene Name TOP1
Species Homo sapiens
Uniprot ID TOP1_HUMAN
Sequence MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKK
HKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEP
EDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKD
KDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKF
YYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC
DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGL
FRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENI
QGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALY
FIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNK
VPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ
QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLAD
ARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSK
LNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 535668New drugs for the treatment of cancer, 1990-2001. Isr Med Assoc J. 2002 Dec;4(12):1124-31.
Ref 541905(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: 6823).
Ref 528447Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer. 2006 Oct;6(10):789-802.
Mutation Info Missense: E710G
Drugs
Drug Name Irinotecan Drug Info [1559263]
Targeted Disease Colorectal cancer
Drug Name Camptothecin Drug Info [1559263]
Targeted Disease Colorectal cancer
Mutation Info Missense: L617H
Drugs
Drug Name Irinotecan Drug Info [1559263]
Targeted Disease Colorectal cancer
Drug Name Camptothecin Drug Info [1559263]
Targeted Disease Colorectal cancer
Mutation Info Missense: R621I
Drugs
Drug Name Irinotecan Drug Info [1559263]
Targeted Disease Colorectal cancer
Drug Name Camptothecin Drug Info [1559263]
Targeted Disease Colorectal cancer
Mutation Info Missense: R634A
Drugs
Drug Name Camptothecin Drug Info [1559270]
Targeted Disease Colorectal cancer
Reference
Ref 1559263New Topoisomerase I mutations are associated with resistance to camptothecin.Mol Cancer.2011 May 27;10:64.
Ref 1559270The human topoisomerase 1B Arg634Ala mutation results in camptothecin resistance and loss of inter-domain motion correlation.Biochim Biophys Acta.2013 Dec;1834(12):2712-21.

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