1fvv
THE STRUCTURE OF CDK2/CYCLIN A IN COMPLEX WITH AN OXINDOLE INHIBITOR
OverviewOverview
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.
About this StructureAbout this Structure
1FVV is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors., Davis ST, Benson BG, Bramson HN, Chapman DE, Dickerson SH, Dold KM, Eberwein DJ, Edelstein M, Frye SV, Gampe Jr RT, Griffin RJ, Harris PA, Hassell AM, Holmes WD, Hunter RN, Knick VB, Lackey K, Lovejoy B, Luzzio MJ, Murray D, Parker P, Rocque WJ, Shewchuk L, Veal JM, Walker DH, Kuyper LF, Science. 2001 Jan 5;291(5501):134-7. PMID:11141566 Page seeded by OCA on Fri May 2 16:49:19 2008
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- Homo sapiens
- Non-specific serine/threonine protein kinase
- Protein complex
- Benson, B G.
- Bramson, H N.
- Chapman, D E.
- Davis, S T.
- Dickerson, S H.
- Dold, K M.
- Eberwein, D J.
- Edelstein, M.
- Frye, S V.
- Griffin, R J.
- Harris, P A.
- Hassell, A M.
- Holmes, W D.
- Hunter, R N.
- Jr., R T.Gampe.
- Knick, V B.
- Kuyper, L K.
- Lackey, K.
- Lovejoy, B.
- Luzzio, M J.
- Murray, D.
- Parker, P.
- Rocque, W J.
- Shewchuk, L.
- Veal, J M.
- Walker, D H.
- Cyclin some
- Cyclin-dependent kinase