Pocket picking: Electrophile-modified quinazolines have been developed as covalent ligands of a lipid binding pocket in p38α, the biological function of which is as yet unknown. Their binding to tailor-made kinase mutants was validated by mass spectrometry and protein X-ray crystallography. This chemical genetic approach led to the identification of specific protein–ligand pairs suitable for application in future studies.

中文翻译：

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针对p38αMAPK突变体的共价脂质口袋配体

口袋采摘：亲电试剂修饰的喹唑啉已开发为p38α中脂质结合口袋的共价配体，其生物学功能尚不清楚。它们与特制激酶突变体的结合已通过质谱和蛋白质X射线晶体学验证。这种化学遗传方法导致鉴定出适用于未来研究的特定蛋白质-配体对。