2v10
From Proteopedia
(New page: 200px<br /> <applet load="2v10" size="450" color="white" frame="true" align="right" spinBox="true" caption="2v10, resolution 3.1Å" /> '''CRYSTAL STRUCTURE OF...) |
|||
| Line 8: | Line 8: | ||
==About this Structure== | ==About this Structure== | ||
| - | 2V10 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 C61 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.15 3.4.23.15]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2V10 OCA]]. | + | 2V10 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 C61 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Renin Renin]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.15 3.4.23.15]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2V10 OCA]]. |
==Reference== | ==Reference== | ||
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin., Rahuel J, Rasetti V, Maibaum J, Rueger H, Goschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grutter MG, Chem Biol. 2000 Jul;7(7):493-504. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=10903938 10903938] | Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin., Rahuel J, Rasetti V, Maibaum J, Rueger H, Goschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grutter MG, Chem Biol. 2000 Jul;7(7):493-504. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=10903938 10903938] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| + | [[Category: Renin]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Cohen, N.C.]] | [[Category: Cohen, N.C.]] | ||
| Line 37: | Line 38: | ||
[[Category: zymogen]] | [[Category: zymogen]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:37:50 2007'' |
Revision as of 10:33, 30 October 2007
|
CRYSTAL STRUCTURE OF RENIN WITH INHIBITOR 9
Overview
BACKGROUND: The aspartic proteinase renin plays an important physiological, role in the regulation of blood pressure. It catalyses the first step in, the conversion of angiotensinogen to the hormone angiotensin II. In the, past, potent peptide inhibitors of renin have been developed, but none of, these compounds has made it to the end of clinical trials. Our primary aim, was to develop novel nonpeptide inhibitors. Based on the available, structural information concerning renin-substrate interactions, we, synthesized inhibitors in which the peptide portion was replaced by, lipophilic moieties that interact with the large hydrophobic S1/S3-binding, pocket in renin. RESULTS: Crystal structure analysis of renin-inhibitor, complexes combined with computational methods were employed in the, ... [(full description)]
About this Structure
2V10 is a [Single protein] structure of sequence from [Homo sapiens] with C61 as [ligand]. Active as [Renin], with EC number [3.4.23.15]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin., Rahuel J, Rasetti V, Maibaum J, Rueger H, Goschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grutter MG, Chem Biol. 2000 Jul;7(7):493-504. PMID:10903938
Page seeded by OCA on Tue Oct 30 12:37:50 2007
Categories: Homo sapiens | Renin | Single protein | Cohen, N.C. | Cumin, F. | Fuhrer, W. | Goschke, R. | Grutter, M.G. | Maibaum, J. | Rahuel, J. | Rasetti, V. | Rueger, H. | Stutz, S. | Wood, J.M. | C61 | Alternative splicing | Aspartyl protease | Cleavage on pair of basic residues | Glycoprotein | Hydrolase | Hydrolase(acid proteinase) | Inhibitor-complex | Polymorphism | Protease | Zymogen
