2bks: Difference between revisions
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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: PZ1]] | [[Category: PZ1]] | ||
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[[Category: zymogen]] | [[Category: zymogen]] | ||
''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 16:38:51 2008'' | ||
Revision as of 17:38, 21 February 2008
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CRYSTAL STRUCTURE OF RENIN-PF00074777 COMPLEX
OverviewOverview
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.
DiseaseDisease
Known diseases associated with this structure: Hyperproreninemia OMIM:[179820], Renal tubular dysgenesis OMIM:[179820]
About this StructureAbout this Structure
2BKS 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.
ReferenceReference
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
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