2bks: Difference between revisions

Revision as of 18:36, 5 November 2007

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.

About this StructureAbout this Structure

2BKS is a Single protein structure of sequence from Homo sapiens with PZ1 as ligand. Active as Renin, with EC number 3.4.23.15 Structure known Active Site: AC1. 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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