| Literature DB >> 11141566 |
S T Davis1, B G Benson, H N Bramson, D E Chapman, S H Dickerson, K M Dold, D J Eberwein, M Edelstein, S V Frye, R T Gampe, R J Griffin, P A Harris, A M Hassell, W D Holmes, R N Hunter, V B Knick, K Lackey, B Lovejoy, M J Luzzio, D Murray, P Parker, W J Rocque, L Shewchuk, J M Veal, D H Walker, L F Kuyper.
Abstract
Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of cyclin-dependent kinase 2 (CDK2), a positive regulator of eukaryotic cell cycle progression, may represent a therapeutic strategy for prevention of chemotherapy-induced alopecia (CIA) by arresting the cell cycle and reducing the sensitivity of the epithelium to many cell cycle-active antitumor agents. Potent small-molecule inhibitors of CDK2 were developed using structure-based methods. Topical application of these compounds in a neonatal rat model of CIA reduced hair loss at the site of application in 33 to 50% of the animals. Thus, inhibition of CDK2 represents a potentially useful approach for the prevention of CIA in cancer patients.Entities:
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Year: 2001 PMID： 11141566 DOI： 10.1126/science.291.5501.134
Source DB: PubMed Journal: Science ISSN： 0036-8075 Impact factor: 47.728