CDK5抑制剂研究进展

Advances in Research on CDK5 Inhibitor

细胞周期蛋白依赖性激酶-5(cyclin-dependent kinase-5,CDK5)是一个多功能的丝氨酸/苏氨酸蛋白激酶,它不参与细胞周期调控,其生理功能主要表现在维持神经细胞的正常发育和有丝分裂后神经细胞的功能及骨架结构。CDK5抑制剂研究备受关注,对治疗神经退化性疾病﹑糖尿病﹑癌症和疼痛具有潜在的疗效。本文对已报道的CDK5抑制剂的结构、与蛋白的作用模式和构效关系进行综述,为合理地设计该类药物提供有益的启示。

Cyclin-dependent kinase-5（CDK5） is a multiftmctional serine/threonine kinase, and doesn＇t regulate cell cycle but mainly participate in maintaining neural development and the function and architecture of adult nerve cell. CDK5 Inhibitors, as new promising drug for the treatment of neurodegenerative diseases, diabetes, cancer and pain etc., are getting more and more attentions. This review has addressed progress of the structures and the SARs of CDK5 inhibitors in recent years, from which prompt for the ideal candidate compounds might be acquired.