Described herein are irreversible kinase inhibitor compounds having the structure:
wherein:
is an active site binding moiety selected from
Y is a linker moiety and G is a Michael acceptor moiety; methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
本文描述的是具有以下结构的不可逆激酶
抑制剂化合物:
其中
是活性位点结合分子,选自
Y是连接分子,G是迈克尔受体分子;合成这种不可逆
抑制剂的方法,以及使用这种不可逆
抑制剂治疗疾病的方法。本文进一步描述了用于确定蛋白质(包括激酶)的适当不可逆
抑制剂的方法、检测方法和系统。