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Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures
- Source :
- European Journal of Medicinal Chemistry. 164:615-639
- Publication Year :
- 2019
- Publisher :
- Elsevier BV, 2019.
-
Abstract
- 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.
- Subjects :
- Protein Data Bank (RCSB PDB)
Crystallography, X-Ray
01 natural sciences
03 medical and health sciences
Cyclin-dependent kinase
Drug Discovery
Animals
Humans
Protein Kinase Inhibitors
030304 developmental biology
Pharmacology
0303 health sciences
Molecular Structure
biology
010405 organic chemistry
Chemistry
Kinase
Organic Chemistry
Biological activity
General Medicine
computer.file_format
Cell cycle
Protein Data Bank
Small molecule
Cyclin-Dependent Kinases
0104 chemical sciences
Cell biology
biology.protein
biological phenomena, cell phenomena, and immunity
computer
CDK inhibitor
Protein Binding
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 164
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....cc221f80bce815ad6db5ec807922d5c4