title: The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
abstract: 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.
authors.affiliation: Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. ntumey@athersys.com
authors.forename: L Nathan
authors.initials: LN
authors.lastname: Tumey
authors.forename: Bayard
authors.initials: B
authors.lastname: Huck
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Gleason
authors.forename: Jianmin
authors.initials: J
authors.lastname: Wang
authors.forename: Daniel
authors.initials: D
authors.lastname: Silver
authors.forename: Kurt
authors.initials: K
authors.lastname: Brunden
authors.forename: Sherry
authors.initials: S
authors.lastname: Boozer
authors.forename: Stephen
authors.initials: S
authors.lastname: Rundlett
authors.forename: Bruce
authors.initials: B
authors.lastname: Sherf
authors.forename: Steven
authors.initials: S
authors.lastname: Murphy
authors.forename: Andrew
authors.initials: A
authors.lastname: Bailey
authors.forename: Tom
authors.initials: T
authors.lastname: Dent
authors.forename: Christina
authors.initials: C
authors.lastname: Leventhal
authors.forename: John
authors.initials: J
authors.lastname: Harrington
authors.forename: Youssef L
authors.initials: YL
authors.lastname: Bennani
mesh_terms: D002087:Butyrates / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D045585:Flap Endonucleases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D002087:Butyrates; D004791:Enzyme Inhibitors; D045585:Flap Endonucleases