Review Article

c-Jun N-末端激酶(JNK)抑制剂的研究进展

卷 28, 期 3, 2021

发表于: 10 February, 2020

页: [607 - 627] 页: 21

弟呕挨: 10.2174/0929867327666200210144114

价格: $65

摘要

c-Jun N-末端激酶(JNKs)是丝裂原活化蛋白激酶(MAPK)信号通路的成员,在许多疾病的发病机制中发挥关键作用,包括癌症、炎症、帕金森病、阿尔茨海默病、心血管疾病、肥胖和糖尿病。因此,JNKs是治疗药物新的优良靶点。在过去的十年中,人们发现了许多基于不同分子支架的JNK抑制剂。然而,只有少数药物进入了临床试验阶段。JNK抑制剂作为治疗药物发展的主要障碍是jnk亚型的选择性。本文综述了JNK抑制剂的最新进展,包括ATP竞争性和ATP非竞争性(别构)抑制剂、双齿结合抑制剂和双齿抑制剂,以及JNK抑制剂作为潜在治疗药物面临的挑战和未来的发展方向。

关键词: JNK,抑制剂,ATP结合位点,JNK亚型选择性,变构,双齿,丝裂原活化蛋白激酶(MAPK)

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