First time at Proteopedia? Click on the green links: they change the 3D image. Click and drag the molecules. Proteopedia is a 3D, interactive encyclopedia of proteins, RNA, DNA and other molecules. With a free user account, you can edit pages in Proteopedia. Visit the Main Page to learn more.
1fvt
From Proteopedia
| 1fvt, resolution 2.20Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Ligands: | |||||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||||
| |||||||||
| |||||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Contents |
THE STRUCTURE OF CYCLIN-DEPENDENT KINASE 2 (CDK2) IN COMPLEX WITH AN OXINDOLE INHIBITOR
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.
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
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
1fvt is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
See Also
Reference
- 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. Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors. Science. 2001 Jan 5;291(5501):134-7. PMID:11141566 doi:10.1126/science.291.5501.134
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | 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. | Gampe, R T. | Griffin, R J. | Harris, P A. | Hassell, A M. | Holmes, W D. | Hunter, R N. | 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. | Cell cycle | Cyclin-dependent kinase | Oxindole | Transferase
