1w51: Difference between revisions
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==Overview== | ==Overview== | ||
Human BACE, also known as beta-secretase, shows promise as a potential | Human BACE, also known as beta-secretase, shows promise as a potential therapeutic target for Alzheimer's disease. We determined the apo structure of BACE to 1.75 A, and a structure of a hydroxyethylamine inhibitor complex derived by soaking. These show significant active-site movements compared to previously described BACE structures. Additionally, the structures reveal two pockets that could be targeted by structure-based drug design. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Cleasby, A.]] | [[Category: Cleasby, A.]] | ||
[[Category: Murray, C | [[Category: Murray, C W.]] | ||
[[Category: Patel, S.]] | [[Category: Patel, S.]] | ||
[[Category: Vuillard, L.]] | [[Category: Vuillard, L.]] | ||
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[[Category: zymogen]] | [[Category: zymogen]] | ||
''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 15:40:33 2008'' | ||
Revision as of 13:40, 21 February 2008
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BACE (BETA SECRETASE) IN COMPLEX WITH A NANOMOLAR NON-PEPTIDIC INHIBITOR
Overview
Human BACE, also known as beta-secretase, shows promise as a potential therapeutic target for Alzheimer's disease. We determined the apo structure of BACE to 1.75 A, and a structure of a hydroxyethylamine inhibitor complex derived by soaking. These show significant active-site movements compared to previously described BACE structures. Additionally, the structures reveal two pockets that could be targeted by structure-based drug design.
About this Structure
1W51 is a Single protein structure of sequence from Homo sapiens with IOD and L01 as ligands. Active as Memapsin 2, with EC number 3.4.23.46 Known structural/functional Site: AC1. Full crystallographic information is available from OCA.
Reference
Apo and inhibitor complex structures of BACE (beta-secretase)., Patel S, Vuillard L, Cleasby A, Murray CW, Yon J, J Mol Biol. 2004 Oct 15;343(2):407-16. PMID:15451669
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