Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275.

Abstract:

: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.

authors

Losiewicz MD,Carlson BA,Kaur G,Sausville EA,Worland PJ

doi

10.1006/bbrc.1994.1742

subject

Has Abstract

pub_date

1994-06-15 00:00:00

pages

589-95

issue

2

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(84)71742-6

journal_volume

201

pub_type

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