The Bruton Tyrosine Kinase (BTK) Inhibitor ACP-196 Demonstrates Clinical Activity in Two Mouse Models of Chronic Lymphocytic Leukemia
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چکیده
منابع مشابه
BTK (Bruton agammaglobulinemia tyrosine kinase)
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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The safety and efficacy of ibrutinib, an oral inhibitor of Bruton tyrosine kinase, were evaluated with chemoimmunotherapy (CIT) in a multicenter phase 1b study. Patients with relapsed/refractory chronic lymphocytic leukemia received bendamustine and rituximab (BR) or fludarabine, cyclophosphamide, and rituximab (FCR) for up to 6 cycles with daily ibrutinib (420 mg) until progressive disease or ...
متن کاملAcalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.
Several small-molecule Bruton tyrosine kinase (BTK) inhibitors are in development for B cell malignancies and autoimmune disorders, each characterized by distinct potency and selectivity patterns. Herein we describe the pharmacologic characterization of BTK inhibitor acalabrutinib [compound 1, ACP-196 (4-[8-amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-(2-pyridyl)benz...
متن کاملAcalabrutinib (ACP-196): a selective second-generation BTK inhibitor
More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton's tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's macroglobulinemia. More selective BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being...
متن کاملThe Importance of Bruton Tyrosine Kinase (BTK) and Targeted Therapies
Submit Manuscript | http://medcraveonline.com (BCR) signalling [6-8], CXCR4 and CXCR5 chemokine receptors, adhesion molecules (integrin), collagen GPVI-FCR gamma chain, GPIB-IX-V complex, CLEC-2 signalling and Toll receptor signalling. BTK is primarily expressed in haematopoietic cells, particularly in B cells, but also in monocytes/macrophages, platelets, neutrophils but not T cells and plasma...
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ژورنال
عنوان ژورنال: Blood
سال: 2015
ISSN: 0006-4971,1528-0020
DOI: 10.1182/blood.v126.23.2920.2920