Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 164, Issue -, Pages 615-639Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.01.003
Keywords
CDK; Inhibitor; Co-crystal structure; Pharmacological activity; Selectivity
Categories
Funding
- National Natural Science Foundation of China [81703417, 31700291]
- Major Science and Technology Project of Henan Province [161100310100]
- Young Scholar Fund from The First Affiliated Hospital of Zhengzhou University
Ask authors/readers for more resources
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. (C) 2019 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available