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    Bioorg Med Chem Lett. 2004 Oct 4;14(19):4915-8.

    The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.

    Tumey LN, Huck B, Gleason E, Wang J, Silver D, Brunden K, Boozer S, Rundlett S, Sherf B, Murphy S, Bailey A, Dent T, Leventhal C, Harrington J, Bennani YL.

    Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. ntumey@athersys.com

    There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors.

    PMID: 15341951 [PubMed - indexed for MEDLINE]

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