SKP2型
激酶
泛素
癌症研究
高通量筛选
细胞周期蛋白依赖激酶
蛋白质亚单位
转移
生物
小分子
化学
细胞周期
细胞生物学
泛素连接酶
癌症
生物化学
细胞
遗传学
基因
作者
Kaizhao Hu,Xiaojing Li,Moges Dessale Asmamaw,Xiaojing Shi,Hong‐Min Liu
标识
DOI:10.1038/s41598-021-00646-3
摘要
Abstract S-phase kinase associated protein 2 (Skp2), a member of the F-box family that constitute the largest known class of ubiquitin E3 specificity components, is responsible for recognizing and recruiting cyclin-dependent kinase inhibitor p27 for its ubiquitination in the presence of the small accessory protein cyclin-dependent kinase regulatory subunit 1(Cks1). Skp2 is overexpressed in esophageal carcinoma tissues and closely related with tumor poor prognosis, and perturbation of the Skp2-Cks1 interaction by inhibitors or RNAi could inhibit the proliferation and metastasis of tumor cells. Therefore, inhibition of Skp2 function by small-molecule compounds targeting Skp2-Cks1 interaction is emerging as a promising and novel anti-cancer strategy. In this study, we establish an improved high-throughput screening platform to screen Skp2 inhibitors targeting Skp2-Cks1interaction, which may provide a new therapeutic approach for the clinic.
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