1xs7
From Proteopedia
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'''Crystal Structure of a cycloamide-urethane-derived novel inhibitor bound to human brain memapsin 2 (beta-secretase).''' | '''Crystal Structure of a cycloamide-urethane-derived novel inhibitor bound to human brain memapsin 2 (beta-secretase).''' | ||
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[[Category: Weerasena, V.]] | [[Category: Weerasena, V.]] | ||
[[Category: Xu, X.]] | [[Category: Xu, X.]] | ||
- | [[Category: | + | [[Category: Acid protease]] |
- | [[Category: | + | [[Category: Alzheimer's disease]] |
- | [[Category: | + | [[Category: Asp2]] |
- | [[Category: | + | [[Category: Aspartic protease]] |
- | [[Category: | + | [[Category: Bace]] |
- | [[Category: | + | [[Category: Beta secretase]] |
- | [[Category: | + | [[Category: Crystallography]] |
- | [[Category: | + | [[Category: Drug design]] |
- | [[Category: | + | [[Category: Memapsin2]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 15:26:46 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 12:26, 3 May 2008
Crystal Structure of a cycloamide-urethane-derived novel inhibitor bound to human brain memapsin 2 (beta-secretase).
Overview
A series of novel macrocyclic amide-urethanes was designed and synthesized based upon the X-ray crystal structure of our lead inhibitor (1, OM99-2 with eight residues) bound to memapsin 2. Ring size and substituent effects have been investigated. Cycloamide-urethanes containing 14- to 16-membered rings exhibited low nanomolar inhibitory potencies against human brain memapsin 2 (beta-secretase).
About this Structure
1XS7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase)., Ghosh AK, Devasamudram T, Hong L, DeZutter C, Xu X, Weerasena V, Koelsch G, Bilcer G, Tang J, Bioorg Med Chem Lett. 2005 Jan 3;15(1):15-20. PMID:15582402 Page seeded by OCA on Sat May 3 15:26:46 2008
Categories: Homo sapiens | Memapsin 2 | Single protein | Bilcer, G. | DeZutter, C. | Devasamudram, T. | Ghosh, A. | Hong, L. | Koelsch, G. | Tang, J. | Weerasena, V. | Xu, X. | Acid protease | Alzheimer's disease | Asp2 | Aspartic protease | Bace | Beta secretase | Crystallography | Drug design | Memapsin2