Journal
EXPERIMENTAL HEMATOLOGY & ONCOLOGY
Volume 3, Issue -, Pages -Publisher
BMC
DOI: 10.1186/2162-3619-3-4
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Funding
- Xiamen Zhongshan Hospital, Fujian, China
- International Scholar Exchange Foundation, US
- NYMC Blood Disease Fund, US
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Research over the role of Bruton's agammaglobulinemia tyrosine kinase (BTK) in B-lymphocyte development, differentiation, signaling and survival has led to better understanding of the pathogenesis of B-cell malignancies. Down-regulation of BTK activity is an attractive novel strategy for treating patients with B-cell malignancies. Ibrutinib (PCI-32765), a potent inhibitor of BTK induces impressive responses in B-cell malignancies through irreversible bond with cysteine-481 in the active site of BTK (TH/SH1 domain) and inhibits BTK phosphorylation on Tyr(223). This review discussed in details the role of BTK in B-cell signaling, molecular interactions between B cell lymphoma/leukemia cells and their microenvironment. Clinical trials of the novel BTK inhibitor, ibrutinib (PCI-32765), in B cell malignancies were summarized.
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