This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
1xs7
From Proteopedia
(New page: 200px<br /> <applet load="1xs7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1xs7, resolution 2.8Å" /> '''Crystal Structure of...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1xs7.gif|left|200px]]<br /> | + | [[Image:1xs7.gif|left|200px]]<br /><applet load="1xs7" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1xs7" size=" | + | |
caption="1xs7, resolution 2.8Å" /> | caption="1xs7, resolution 2.8Å" /> | ||
'''Crystal Structure of a cycloamide-urethane-derived novel inhibitor bound to human brain memapsin 2 (beta-secretase).'''<br /> | '''Crystal Structure of a cycloamide-urethane-derived novel inhibitor bound to human brain memapsin 2 (beta-secretase).'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A series of novel macrocyclic amide-urethanes was designed and synthesized | + | 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== | ==About this Structure== | ||
| - | 1XS7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MMI as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] Full crystallographic information is available from [http:// | + | 1XS7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MMI:'>MMI</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XS7 OCA]. |
==Reference== | ==Reference== | ||
| Line 35: | Line 34: | ||
[[Category: memapsin2]] | [[Category: memapsin2]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:58:07 2008'' |
Revision as of 13:58, 21 February 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 with 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 Thu Feb 21 15:58:07 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. | MMI | Acid protease | Alzheimer's disease | Asp2 | Aspartic protease | Bace | Beta secretase | Crystallography | Drug design | Memapsin2
