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.


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




Has Abstract


1994-06-15 00:00:00














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    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: De Stasio PR,Taylor MW

    更新日期:1989-03-15 00:00:00

  • Effect of ELOVL3 expression on bovine skeletal muscle-derived satellite cell differentiation.

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Chen K,Inoue M,Okada A

    更新日期:1996-07-25 00:00:00

  • Presence of dioxins in human follicular fluid: their possible stage-specific action on the development of preimplantation mouse embryos.

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

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    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Morita A,Suzuki N,Matsumoto Y,Hirano K,Enomoto A,Zhu J,Sakai K

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    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Díaz A,Humeres C,González V,Gómez MT,Montt N,Sanchez G,Chiong M,García L

    更新日期:2015-11-13 00:00:00