Resistance mutation info of target

Target General Information
Target ID T25005
Target Name Tyrosine-protein kinase BTK (BTK) Target Info
Gene Name BTK
Species Homo sapiens
Uniprot ID BTK_HUMAN
Sequence MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEK
ITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEEL
RKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSS
HRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDE
YFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGK
EGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELIN
YHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGK
WRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANG
CLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDF
GLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYER
FTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
[Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 524263ClinicalTrials.gov (NCT01833039) An Open Label Treatment Use Protocol for Ibrutinib in Subjects With Relapsed or Refractory Mantle Cell Lymphoma. U.S. National Institutes of Health.
Ref 541962(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: 6912).
Ref 551043Janssen's IMBRUVICA (ibrutinib) Receives Additional European Commission Approval for the Treatment of Waldenstrom's Macroglobulinemia. Janssen-Cilag International NV (Janssen). Jul 10, 2015.
Mutation Info Missense: C481S
Drugs
Drug Name Ibrutinib Drug Info [556014], [556126]
Targeted Disease Refractory hematologic malignancy
Mutation Prevalence 2.60% of the patients
Drug Name Ibrutinib Drug Info [556014], [556126]
Targeted Disease Refractory hematologic malignancy
Mutation Prevalence 2.60% of the patients
Reference
Ref 556014Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib. N Engl J Med. 2014 Jun 12;370(24):2286-94. doi: 10.1056/NEJMoa1400029. Epub 2014 May 28.
Ref 556126Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition. Nat Commun. 2016 May 20;7:11589. doi: 10.1038/ncomms11589.

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