1bim
From Proteopedia
(New page: 200px<br /> <applet load="1bim" size="450" color="white" frame="true" align="right" spinBox="true" caption="1bim, resolution 2.8Å" /> '''CRYSTALLOGRAPHIC STU...) |
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| - | [[Image:1bim.gif|left|200px]]<br /> | + | [[Image:1bim.gif|left|200px]]<br /><applet load="1bim" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1bim" size=" | + | |
caption="1bim, resolution 2.8Å" /> | caption="1bim, resolution 2.8Å" /> | ||
'''CRYSTALLOGRAPHIC STUDIES ON THE BINDING MODES OF P2-P3 BUTANEDIAMIDE RENIN INHIBITORS'''<br /> | '''CRYSTALLOGRAPHIC STUDIES ON THE BINDING MODES OF P2-P3 BUTANEDIAMIDE RENIN INHIBITORS'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The binding modes of three peptidomimetic P2-P3 butanediamide renin | + | The binding modes of three peptidomimetic P2-P3 butanediamide renin inhibitors have been determined by x-ray crystallography. The inhibitors are bound with their backbones in an extended conformation, and their side chains occupying the S5 to S1' pockets. A (2-amino-4-thiazolyl)methyl side chain at the P2 position shows stronger hydrogen-bonding and van der Waals interactions with renin than the His side chain, which is present in the natural substrate. The ACHPA-gamma-lactam transition state analog has similar interactions with renin as the dihydroxyethylene transition state analog. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1BIM 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 DMF, PHC, HII and IP4 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1BIM 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=DMF:'>DMF</scene>, <scene name='pdbligand=PHC:'>PHC</scene>, <scene name='pdbligand=HII:'>HII</scene> and <scene name='pdbligand=IP4:'>IP4</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BIM OCA]. |
==Reference== | ==Reference== | ||
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[[Category: aspartic proteinase]] | [[Category: aspartic proteinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 11:55:42 2008'' |
Revision as of 09:55, 21 February 2008
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CRYSTALLOGRAPHIC STUDIES ON THE BINDING MODES OF P2-P3 BUTANEDIAMIDE RENIN INHIBITORS
Contents |
Overview
The binding modes of three peptidomimetic P2-P3 butanediamide renin inhibitors have been determined by x-ray crystallography. The inhibitors are bound with their backbones in an extended conformation, and their side chains occupying the S5 to S1' pockets. A (2-amino-4-thiazolyl)methyl side chain at the P2 position shows stronger hydrogen-bonding and van der Waals interactions with renin than the His side chain, which is present in the natural substrate. The ACHPA-gamma-lactam transition state analog has similar interactions with renin as the dihydroxyethylene transition state analog.
Disease
Known diseases associated with this structure: Hyperproreninemia OMIM:[179820], Renal tubular dysgenesis OMIM:[179820]
About this Structure
1BIM is a Single protein structure of sequence from Homo sapiens with , , and as ligands. Full crystallographic information is available from OCA.
Reference
Crystallographic studies on the binding modes of P2-P3 butanediamide renin inhibitors., Tong L, Pav S, Lamarre D, Simoneau B, Lavallee P, Jung G, J Biol Chem. 1995 Dec 8;270(49):29520-4. PMID:7493993
Page seeded by OCA on Thu Feb 21 11:55:42 2008
Categories: Homo sapiens | Single protein | Tong, L. | DMF | HII | IP4 | PHC | Aspartic proteinase
