Year: 2009
Type: article
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.
Source: Biochemistry
DOI: 10.1021/bi901061a
Authors: Robert Godemann, James Madden, Joachim Krämer, Myron Smith, Ulrike Fritz, Thomas Hesterkamp, John Barker, Sabine Höppner, David Hallett, Andrea Cesura, Andreas Ebneth, John Kemp
Institutions: Evotec (Germany), Evotec (United Kingdom)
Language: English
Subfield: Cellular and Molecular Neuroscience
Field: Neuroscience
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W200948446