Tumey L Nathan, Huck Bayard, Gleason Elizabeth, Wang Jianmin, Silver Daniel, Brunden Kurt, Boozer Sherry, Rundlett Stephen, Sherf Bruce, Murphy Steven, Bailey Andrew, Dent Tom, Leventhal Christina, Harrington John, Bennani Youssef L
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA.
Bioorg Med Chem Lett. 2004 Oct 4;14(19):4915-8. doi: 10.1016/j.bmcl.2004.07.028.
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.
最近有几篇关于通过抑制DNA修复过程实现化学增敏作用的报道。翼状内切核酸酶1(FEN1)是参与碱基切除修复(BER)的关键酶,碱基切除修复是哺乳动物细胞用于修复DNA损伤的主要途径。在本报告中,我们描述了一系列2,4-二酮丁酸FEN1抑制剂的鉴定及其构效关系。