酪蛋白激酶2
三磷酸腺苷
药物发现
激酶
苏氨酸
丝氨酸
生物化学
酪蛋白激酶1
蛋白激酶A
化学
酶
计算生物学
生物
细胞周期蛋白依赖激酶2
作者
Shivani Patel,Vivek K. Vyas,Manmohan Sharma,Manjunath Ghate
出处
期刊:Future Medicinal Chemistry
[Newlands Press Ltd]
日期:2023-06-01
卷期号:15 (11): 987-1014
标识
DOI:10.4155/fmc-2023-0005
摘要
Casein kinase 2 (CK2) is a ubiquitous, highly pleiotropic serine-threonine kinase. CK2 has been identified as a potential drug target for the treatment of cancer and related disorders. Several adenosine triphosphate-competitive CK2 inhibitors have been identified and have progressed at different levels of clinical trials. This review presents details of CK2 protein, structural insights into adenosine triphosphate binding pocket, current clinical trial candidates and their analogues. Further, it includes the emerging structure-based drug design approaches, chemistry, structure–activity relationship and biological screening of potent and selective CK2 inhibitors. The authors tabulated the details of CK2 co-crystal structures because these co-crystal structures facilitated the structure-guided discovery of CK2 inhibitors. The narrow hinge pocket compared with related kinases provides useful insights into the discovery of CK2 inhibitors.
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