2bkt
From Proteopedia
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==Overview== | ==Overview== | ||
| - | We have found that both enantiomeric configurations of the | + | We have found that both enantiomeric configurations of the 6-alkoxymethyl-1-aryl-2-piperazinone scaffold display equipotent renin inhibition activity and similar SAR patterns. This enantiomeric flexibility is in contrast to a previously reported 3-alkoxymethyl-4-arylpiperidine scaffold. |
==Disease== | ==Disease== | ||
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[[Category: Renin]] | [[Category: Renin]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Bryant, J | + | [[Category: Bryant, J W.]] |
| - | [[Category: Clay, E | + | [[Category: Clay, E H.]] |
| - | [[Category: Edmunds, J | + | [[Category: Edmunds, J J.]] |
| - | [[Category: Holsworth, D | + | [[Category: Holsworth, D D.]] |
[[Category: Jalaie, M.]] | [[Category: Jalaie, M.]] | ||
| - | [[Category: Powell, N | + | [[Category: Powell, N A.]] |
| - | [[Category: Ryan, J | + | [[Category: Ryan, J M.]] |
[[Category: Zhang, E.]] | [[Category: Zhang, E.]] | ||
[[Category: RPF]] | [[Category: RPF]] | ||
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[[Category: renin]] | [[Category: renin]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:38:52 2008'' |
Revision as of 14:38, 21 February 2008
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CRYSTAL STRUCTURE OF RENIN-PF00257567 COMPLEX
Contents |
Overview
We have found that both enantiomeric configurations of the 6-alkoxymethyl-1-aryl-2-piperazinone scaffold display equipotent renin inhibition activity and similar SAR patterns. This enantiomeric flexibility is in contrast to a previously reported 3-alkoxymethyl-4-arylpiperidine scaffold.
Disease
Known diseases associated with this structure: Hyperproreninemia OMIM:[179820], Renal tubular dysgenesis OMIM:[179820]
About this Structure
2BKT is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Renin, with EC number 3.4.23.15 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors., Powell NA, Clay EH, Holsworth DD, Bryant JW, Ryan MJ, Jalaie M, Zhang E, Edmunds JJ, Bioorg Med Chem Lett. 2005 May 2;15(9):2371-4. PMID:15837327
Page seeded by OCA on Thu Feb 21 16:38:52 2008
Categories: Homo sapiens | Renin | Single protein | Bryant, J W. | Clay, E H. | Edmunds, J J. | Holsworth, D D. | Jalaie, M. | Powell, N A. | Ryan, J M. | Zhang, E. | RPF | Aspartyl protease | Hydrolase
