Document Detail

Effects of structurally related flavonoids on cell cycle progression of human melanoma cells: regulation of cyclin-dependent kinases CDK2 and CDK1.
MedLine Citation:
PMID:  11322924     Owner:  NLM     Status:  MEDLINE    
We have investigated the effects of a series of flavonoids on cell proliferation and cell cycle distribution in human melanoma cells OCM-1. Among the compounds that potently inhibited OCM-1 cell proliferation, we show that the presence of a hydroxyl group at the 3'-position of the ring B in quercetin and luteolin, correlated to a G1 cell cycle arrest while its absence in kaempferol and apigenin correlated to a G2 block. Genistein with a hydroxyl at 5-position of the ring A arrested cells in G2 while daidzein which lacks it, induced an accumulation of cells in G1. We demonstrate that flavonoids, which induced a cell cycle block in G1, inhibited the activity of CDK2 by 40-60%. By contrast, those which caused an accumulation of cells in G2/M were without effect. On the other hand, while quercetin, daidzein and luteolin did not alter the activity of CDK1, kaempferol, apigenin and genistein inhibited this kinase by 50-70%. We demonstrate that the up-regulation of the CDK inhibitors p27(KIP1) and p21(CIP1) is likely responsible for the inhibition of CDK2 while inhibition of CDK1 was rather due to the phosphorylation of the kinase on Tyr15 residue.
F Casagrande; J M Darbon
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biochemical pharmacology     Volume:  61     ISSN:  0006-2952     ISO Abbreviation:  Biochem. Pharmacol.     Publication Date:  2001 May 
Date Detail:
Created Date:  2001-04-27     Completed Date:  2001-05-24     Revised Date:  2012-06-25    
Medline Journal Info:
Nlm Unique ID:  0101032     Medline TA:  Biochem Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  1205-15     Citation Subset:  IM    
Laboratoire de Biologie Cellulaire et Moléculaire du Contrôle de la Prolifération, UMR 5088 CNRS, Université Paul Sabatier, 118 route de Narbonne, F-31062 cedex, Toulouse, France
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MeSH Terms
CDC2 Protein Kinase / metabolism*
CDC2-CDC28 Kinases*
Cell Cycle / drug effects
Cell Cycle Proteins*
Cell Division / drug effects
Cyclin-Dependent Kinase 2
Cyclin-Dependent Kinase Inhibitor p21
Cyclin-Dependent Kinase Inhibitor p27
Cyclin-Dependent Kinases / metabolism*
Cyclins / metabolism
Flavonoids / chemistry,  pharmacology*
Gene Expression Regulation, Enzymologic / drug effects*
Melanoma / pathology*
Microtubule-Associated Proteins / metabolism
Phosphorylation / drug effects
Protein-Serine-Threonine Kinases / metabolism*
Structure-Activity Relationship
Tumor Cells, Cultured
Tumor Suppressor Proteins*
Up-Regulation / drug effects
Reg. No./Substance:
0/CDKN1A protein, human; 0/Cell Cycle Proteins; 0/Cyclin-Dependent Kinase Inhibitor p21; 0/Cyclins; 0/Flavonoids; 0/Microtubule-Associated Proteins; 0/Tumor Suppressor Proteins; 147604-94-2/Cyclin-Dependent Kinase Inhibitor p27; EC Kinases; EC Protein Kinase; EC Kinases; EC protein, human; EC Kinase 2; EC Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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