2bks
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, resolution 2.2Å | |||||||
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Sites: | |||||||
Ligands: | |||||||
Activity: | Renin, with EC number 3.4.23.15 | ||||||
Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
Coordinates: | save as pdb, mmCIF, xml |
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. 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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