细胞周期蛋白依赖激酶
激酶
化学
CDK抑制剂
丝氨酸
苏氨酸
细胞周期蛋白
小分子
细胞生物学
生物化学
细胞周期
磷酸化
生物
细胞
作者
Weiyan Cheng,Zhiheng Yang,Suhua Wang,Ying Li,Wei Han,Xin Tian,Quancheng Kan
标识
DOI:10.1016/j.ejmech.2019.01.003
摘要
The cyclin-dependent protein kinases (CDKs) are protein-serine/threonine kinases that display crucial effects in regulation of cell cycle and transcription. While the excessive expression of CDKs is intimate related to the development of diseases including cancers, which provides opportunities for disease treatment. A large number of small molecules are explored targeting CDKs. CDK/inhibitor co-crystal structures play an important role during the exploration of inhibitors. So far nine kinds of CDK/inhibitor co-crystals have been determined, they account for the highest proportion among the Protein Data Bank (PDB) deposited crystal structures. Herein, we review main co-crystals of CDKs in complex with corresponding inhibitors reported in recent years, focusing our attention on the binding models and the pharmacological activities of inhibitors.
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