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Review
, 3 (10), 135

Roscovitine in Cancer and Other Diseases

Affiliations
Review

Roscovitine in Cancer and Other Diseases

Jonas Cicenas et al. Ann Transl Med.

Abstract

Roscovitine [CY-202, (R)-Roscovitine, Seliciclib] is a small molecule that inhibits cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a broad-range purine inhibitor, which inhibits CDK1, CDK2, CDK5 and CDK7, but is a poor inhibitor for CDK4 and CDK6. Roscovitine is widely used as a biological tool in cell cycle, cancer, apoptosis and neurobiology studies. Moreover, it is currently evaluated as a potential drug to treat cancers, neurodegenerative diseases, inflammation, viral infections, polycystic kidney disease and glomerulonephritis. This review focuses on the use of roscovitine in the disease model as well as clinical model research.

Keywords: Cyclin-dependent kinases (CDK); cancer; kidney diseases; neurodegeneration; roscovitine; small molecule inhibitor.

Figures

Figure 1
Figure 1
Roscovitine.
Figure 2
Figure 2
Crystal structure of CDK2 in complex with roscovitine. Image from the RCSB PDB (www.rcsb.org). DOI: 10.2210/pdb2a4l/pdb (19).
Figure 3
Figure 3
Crystal structure of CDK5-p25 in complex with roscovitine. Image from the RCSB PDB (www.rcsb.org). DOI: 10.2210/pdb1unl/pdb (23).
Figure 4
Figure 4
Crystal structure of pyridoxal kinase in complex with roscovitine. Image from the RCSB PDB (www.rcsb.org). DOI: 10.2210/pdb1ygk/pdb (24).
Figure 5
Figure 5
Compounds CR8, DRF053, N-&-N1 and LGR1406.
Figure 6
Figure 6
Compounds 11, 12, 19, 21 and 21.

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