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Article

Fragment-based discovery of nonpeptidic BACE-1 inhibitors using tethering.

Biochemistry - 2 Jun 2009

Yang Wenjin, Fucini Raymond V, Fahr Bruce T, Randal Mike, Lind Kenneth E, Lam Melissa B, Lu Wanli, Lu Yafan, Cary Douglas R, Romanowski Michael J, Colussi Dennis, Pietrak Beth, Allison Timothy J, Munshi Sanjeev K, Penny David M, Pham Phuongly, Sun Jian, Thomas Anila E, Wilkinson Jennifer M, Jacobs Jeffrey W, McDowell Robert S, Ballinger Marcus D

Abstract excerpt

BACE-1 (beta-site amyloid precursor protein cleaving enzyme), a prominent target in Alzheimer's disease drug discovery efforts, was surveyed using Tethering technology to discover small molecule fragment ligands that bind to the enzyme active site. Screens of a library of >15000 thiol-containing fragments versus a panel of BACE-1 active site cysteine mutants under redox-controlled conditions revealed several...

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PMID: 19284778
DOI: 10.1021/bi900017q

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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