2bkt

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[[Category: renin]]
[[Category: renin]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 14:07:27 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 16:40:54 2007''

Revision as of 14:36, 30 October 2007

Image:2bkt.gif

2bkt, resolution 2.3Å

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CRYSTAL STRUCTURE OF RENIN-PF00257567 COMPLEX

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.

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

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