Comparative Analysis of BTK Inhibitors and ... | 合法藥品大搜索

由HYEstupiñán著作·2021·被引用4次—Ibrutinib(Imbruvica®),thefirst-in-classBTKinhibitor(BTKi),isanirreversiblebinder,whichhasrevolutionizedthetherapeuticlandscapeforB- ...

The understanding of the B-cell receptor (BCR) signaling pathway led to the deciphering of the central role of Bruton’s tyrosine kinase (BTK) and the importance of its inhibition as an effective strategy for the treatment of B-cell malignancies (Herman et al., 2011[1]; Smith, 2017[2]; Pal Singh et al., 2018[3]; Lucas and Woyach, 2019[4]). BTK is a non-receptor protein-tyrosine kinase that belongs to the TEC family of kinases. Upon BCR stimulation BTK gets phosphorylated by the SRC-family kinase LYN, and activated BTK phosphorylates its substrate, the downstream molecule phospholipase C-γ2, which results in an increased level of intracellular calcium and activation of transcription factors involved in B-cell proliferation, differentiation and survival (Smith et al., 2001[5]). BTK is expressed in all hematopoietic cells such as macrophages, neutrophils and mast cells, with the exception of T- and plasma cells (...