Second-generation inhibitors of Bruton tyrosine kinase
نویسندگان
چکیده
منابع مشابه
Second-generation inhibitors of Bruton tyrosine kinase
Bruton tyrosine kinase (BTK) is a critical effector molecule for B cell development and plays a major role in lymphoma genesis. Ibrutinib is the first-generation BTK inhibitor. Ibrutinib has off-target effects on EGFR, ITK, and Tec family kinases, which explains the untoward effects of ibrutinib. Resistance to ibrutinib was also reported. The C481S mutation in the BTK kinase domain was reported...
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The BTK protein is a 77 kDa protein of 659 amino acids. Translation of the BTK transcript starts at the ATG site that is located in exon 2 and ends in exon 19. The BTK protein is composed of an N-terminal Pleckstrin homology (PH) domain followed three protein interacting domains: Tec homology (TH) region, Src homology 3 (SH3) domain and SH2 domain. A tyrosine-kinase catalytic domain is located ...
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ژورنال
عنوان ژورنال: Journal of Hematology & Oncology
سال: 2016
ISSN: 1756-8722
DOI: 10.1186/s13045-016-0313-y