Progress in the study of new cancer target Cdk5 and its inhibitors

VernacularTitle:Cdk5-肿瘤新靶点及其抑制剂研究进展
Author: Long-xing MIAO ¹ ; Yi-jun YANG ¹ ; Ze-yu WANG ¹ ; Qian-bin LI ¹ ; Gao-yun HU ¹
Author Information

1. School of Pharmaceutical Sciences, Central South University, Changsha 410013, China
Publication Type:REVIEWS
Keywords: Cdk5; tumor; inhibitor
From: Acta Pharmaceutica Sinica 2016;51(2):226-
CountryChina
Language:Chinese
Abstract: Cyclin-dependent kinase-5 (Cdk5) is a kind of Ser/Thr kinases in the signaling pathway, which regulates the neural development. The recent studies have confirmed that hyperactivation of Cdk5 is closely associated with the evolution, progression and apoptosis of tumors. The Cdk5 inhibitors have been extensively studied in the drug discovery against cancer. The structure features of these inhibitors and molecular mechanisms of their activities have provided clues for the drug development. In the second generation Cdk5 inhibitors, the ATP-binding pocket, a highly conserved site, has been targeted in the drug design in most cases. In addition, a growing number of peptides has been generated by targeting the protein/protein interfaces of Cdk5.