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Chin LS, Murray SF, Doherty PF, Singh SK.
K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c.
Cancer Invest. 1999;17(6):391-5.
Department of Neurosurgery, University of Maryland School of
Medicine, Baltimore, USA.
lchin@surgery1.umaryland.edu
The indole carbazole K252a has been shown in previous studies to
inhibit the platelet-derived growth factor signal transduction
pathway in gliomas. Because K252a has nonspecific effects on
protein kinase function, we studied its effect on
cyclin-dependent kinases (CDK) and cell cycle blockade in glioma
cells. K252a blocked T98G cells at the G1/S and G2/M
checkpoints. Consistent with cell cycle arrest, K252a was shown
to hypophosphorylate Rb, upregulate p21, and decrease Cdc2 and
Cdc25c activity. Finally, cell cycle arrest in T98G cells
resulted in apoptosis as determined by cell morphology and DNA
laddering. K252a is a useful tool for studying the effects of
CDK inhibition and cell cycle blockade in tumor cells.
PMID: 10434949 |
