1xs7
From Proteopedia
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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 with MMI as ligand. Active as Memapsin 2, with EC number 3.4.23.46 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 Mon Nov 12 20:10:12 2007
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. | MMI | Acid protease | Alzheimer's disease | Asp2 | Aspartic protease | Bace | Beta secretase | Crystallography | Drug design | Memapsin2
