2bkt
From Proteopedia
| Line 6: | Line 6: | ||
==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=179820 179820]], Renal tubular dysgenesis OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=179820 179820]] | ||
==About this Structure== | ==About this Structure== | ||
| Line 28: | Line 31: | ||
[[Category: renin]] | [[Category: renin]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:03:53 2007'' |
Revision as of 18:57, 12 November 2007
|
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 RPF 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
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 Mon Nov 12 21:03:53 2007
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
