2b8l: Difference between revisions
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==Overview== | ==Overview== | ||
We have synthesized and evaluated a series of conformationally biased P3 | 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== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Kuo, L.]] | [[Category: Kuo, L.]] | ||
[[Category: Munshi, S | [[Category: Munshi, S K.]] | ||
[[Category: 5HA]] | [[Category: 5HA]] | ||
[[Category: aspartyl protease]] | [[Category: aspartyl protease]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:35:13 2008'' | ||
Revision as of 17:35, 21 February 2008
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Crystal structure of human beta secretase complexed with inhibitor
OverviewOverview
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 StructureAbout this Structure
2B8L is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Memapsin 2, with EC number 3.4.23.46 Full crystallographic information is available from OCA.
ReferenceReference
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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