BTK
Bruton's tyrosine kinase (abbreviated Btk or BTK) also known as tyrosine-protein kinase BTK is an enzyme that in humans is encoded by the BTK gene. BTK plays a crucial role in B cell maturation as well as mast cell activation through the high-affinity IgE receptor.
Btk contains a PH domain that binds phosphatidylinositol (3,4,5)-trisphosphate (PIP3). PIP3 binding induces Btk to phosphorylate phospholipase C, which in turn hydrolyzes PIP2, a phosphatidylinositol, into two second messengers, inositol triphosphate (IP3) and diacylglycerol (DAG), which then go on to modulate the activity of downstream proteins during B-cell signalling.
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LFM-A13是Btk激酶选择性抑制剂，IC50值为17.2uM，也对PLK3有抑制作用。
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CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
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AVL-292是共价结合的，高选择性口服活性Btk抑制剂，IC50为0.5 nM，比对其它激酶的抑制性高1400倍以上。
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CNX-774是口服活性的高效Btk抑制剂，IC50< 1 nM，能与活性位点上的Cys-481形成配体导向的共价键。
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