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Biochemistry. 2009 Nov 17;48(45):10743-51. doi: 10.1021/bi901061a.

Fragment-based discovery of BACE1 inhibitors using functional assays.

Author information

1
Evotec AG, Schnackenburgallee 114, 22525 Hamburg, Germany. robert.godemann@evotec.com

Abstract

Novel nonpeptidic inhibitors of beta-secretase (BACE1) have been discovered by employing a fragment-based biochemical screening approach. A diverse library of 20000 low-molecular weight compounds were screened and yielded 26 novel hits that were confirmed by biochemical and surface plasmon resonance secondary assays. We describe here fragment inhibitors cocrystallized with BACE1 in a flap open and flap closed conformation as determined by X-ray crystallography.

PMID:
19799414
DOI:
10.1021/bi901061a
[Indexed for MEDLINE]

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