1FVV: The Structure Of Cdk2/cyclin A In Complex With An Oxindole Inhibitor

Citation:
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.
PDB ID: 1FVVDownload
MMDB ID: 15424
PDB Deposition Date: 2000/9/20
Updated in MMDB: 2017/10
Experimental Method:
x-ray diffraction
Resolution: 2.8  Å
Source Organism:
Similar Structures:
Biological Unit for 1FVV: dimeric; determined by author and by software (PISA)
Molecular Components in 1FVV
Label Count Molecule
Proteins (2 molecules)
1
Cyclin-dependent Kinase 2(Gene symbol: CDK2)
Molecule annotation
1
Cyclin a(Gene symbol: CCNA2)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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