Journal
DRUG RESISTANCE UPDATES
Volume 3, Issue 2, Pages 83-88Publisher
CHURCHILL LIVINGSTONE
DOI: 10.1054/drup.2000.0129
Keywords
cyclin-dependent kinase; protein kinase inhibitors; cell cycle; Alzheimer's disease; apoptosis; anticancer agents; antineurodegenerative agents; antiviral agents; antiparasitic agents
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Cyclin-dependent kinases (CDKs) play a key role in the cell division cycle, in neuronal functions, in transcription and in apoptosis. Intensive screening with these kinases as targets has lead to the identification of highly selective and potent small - molecule inhibitors. Go-crystallization with CDK2 shows that these flat heterocyclic hydrophobic compounds bind through two or three hydrogen bonds with the side chains of two amino acids located in the ATP-binding pocket of the kinase. These inhibitors are anti-proliferative; they arrest cells in G I and in G2/M phase. Furthermore they facilitate or even trigger apoptosis in proliferating cells while they protect neuronal cells and thymocytes from apoptosis. The potential use of these inhibitors is being extensively evaluated for cancer chemotherapy and also in other therapeutic areas: neurology (Alzheimer's disease), cardiovascular (restenosis, angiogenesis), nephrology (glomerulonephritis), parasitology (Plasmodium, Tryphanosoma, Toxoplasma, etc.) and virology (cytomegalovirus, HIV, herpes virus). (C) 2000 Harcourt Publishers Ltd.
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