Potent Inhibition of Cdc2 Kinase Activity by the Flavonoid L86-8275
Copyright policy )Potent Inhibition of Cdc2 Kinase Activity by the Flavonoid L86-8275
L86-8275 [(-) cis-5,7-dihydroxy-2-(2-chlorophenyl)-8[4-(3-hydroxy-1- methyl)-piperidinyl]-4H-benzopyran-4-one] directly inhibits immunoprecipitated Cdc2 kinase activity from G2/M synchronized MDA-MB-468 breast carcinoma cells and is at least 250-fold more potent than either quercetin or genistein. Purified sea-star Cdc2 kinase (IC50 = 0.5 microM) was inhibited with a similar potency to immunoprecipitated Cdc2 kinase from MDA-MB-468 cells (IC50 = 0.4 microM). This inhibition was competitive with respect to ATP (KiATP = 0.041 microM) and noncompetitive with respect to a synthetic peptide substrate, CDK1S1 (AAKAKKTPKKAKK-CONH2, KiCDK1S1 = 0.14 microM). These data suggest L86-8275 as a lead structure for the development of inhibitors of the cyclin-dependent kinases.
- National Cancer Institute United States
Flavonoids, G2 Phase, Molecular Structure, Molecular Sequence Data, Mitosis, Breast Neoplasms, Protein-Tyrosine Kinases, Genistein, Isoflavones, Growth Inhibitors, Substrate Specificity, Kinetics, Adenosine Triphosphate, Piperidines, CDC2 Protein Kinase, Humans, Female, Quercetin, Amino Acid Sequence, Peptides
Flavonoids, G2 Phase, Molecular Structure, Molecular Sequence Data, Mitosis, Breast Neoplasms, Protein-Tyrosine Kinases, Genistein, Isoflavones, Growth Inhibitors, Substrate Specificity, Kinetics, Adenosine Triphosphate, Piperidines, CDC2 Protein Kinase, Humans, Female, Quercetin, Amino Acid Sequence, Peptides
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