2b8l

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(New page: 200px<br /> <applet load="2b8l" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b8l, resolution 1.7&Aring;" /> '''Crystal structure of...)
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Revision as of 18:53, 12 November 2007

Image:2b8l.gif

2b8l, resolution 1.7Å

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Crystal structure of human beta secretase complexed with inhibitor

Overview

We have synthesized and evaluated a series of conformationally biased P3, amide replacements based on an isophthalamide lead structure. The studies, resulted in the identification of the beta-secretase inhibitor 7m which, has an in vitro IC(50)=35 nM. The synthesis and biological activities of, these compounds are described.

About this Structure

2B8L is a Single protein structure of sequence from Homo sapiens with 5HA as ligand. Active as Memapsin 2, with EC number 3.4.23.46 Full crystallographic information is available from OCA.

Reference

Conformationally biased P3 amide replacements of beta-secretase inhibitors., Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2. PMID:16263281

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