2qzl

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Image:2qzl.jpg

Template:STRUCTURE 2qzl

Crystal Structure of human Beta Secretase complexed with IXS


Overview

A series of beta-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a psi(CH2NH) reduced amide bond were synthesized. Incorporation of this reduced amide isostere as a non-cleavable peptide surrogate afforded inhibitors possessing low nanomolar potencies in both an enzymatic and cell-based assay.

About this Structure

2QZL is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres., Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. Epub 2006 May 11. PMID:16690314 Page seeded by OCA on Thu Apr 24 09:41:43 2008

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