Mitogen-activated protein kinase kinase 7 (MAP2K7) in the c-Jun N-terminal kinase signal cascade is an attractive drug target for a variety of diseases. The selectivity of MAP2K7 inhibitors against off-target kinases is a major barrier in drug development. We report a crystal structure of MAP2K7 complexed with a potent covalent inhibitor bearing an acrylamide moiety as an electrophile, which discloses a structural basis for producing selective and potent MAP2K7 inhibitors.

中文翻译：

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生产选择性MAP2K7抑制剂的结构基础。

c-Jun N末端激酶信号级联反应中的丝裂素活化蛋白激酶7（MAP2K7）是多种疾病的诱人药物靶标。MAP2K7抑制剂对脱靶激酶的选择性是药物开发的主要障碍。我们报告了MAP2K7的晶体结构，该晶体与带有丙烯酰胺部分的强效共价抑制剂（作为亲电子试剂）复合，从而揭示了生产选择性和强效MAP2K7抑制剂的结构基础。