1jje
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(New page: 200px<br /><applet load="1jje" size="450" color="white" frame="true" align="right" spinBox="true" caption="1jje, resolution 1.80Å" /> '''IMP-1 METALLO BETA-L...)
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Revision as of 16:12, 20 November 2007
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IMP-1 METALLO BETA-LACTAMASE FROM PSEUDOMONAS AERUGINOSA IN COMPLEX WITH A BIARYL SUCCINIC ACID INHIBITOR (11)
Overview
IMP-1 metallo-beta-lactamase (class B) is a plasmid-borne zinc, metalloenzyme that efficiently hydrolyzes beta-lactam antibiotics, including carbapenems, rendering them ineffective. Because IMP-1 has been, found in several clinically important carbapenem-resistant pathogens, there is a need for inhibitors of this enzyme that could protect broad, spectrum antibiotics such as imipenem from hydrolysis and thus extend, their utility. We have identified a series of 2,3-(S,S)-disubstituted, succinic acids that are potent inhibitors of IMP-1. Determination of high, resolution crystal structures and molecular modeling of succinic acid, inhibitor complexes with IMP-1 has allowed an understanding of the, potency, stereochemistry, and structure-activity relationships of these, inhibitors.
About this Structure
1JJE is a Single protein structure of sequence from Pseudomonas aeruginosa with ZN, ACT and BYS as ligands. Active as Beta-lactamase, with EC number 3.5.2.6 Full crystallographic information is available from OCA.
Reference
Succinic acids as potent inhibitors of plasmid-borne IMP-1 metallo-beta-lactamase., Toney JH, Hammond GG, Fitzgerald PM, Sharma N, Balkovec JM, Rouen GP, Olson SH, Hammond ML, Greenlee ML, Gao YD, J Biol Chem. 2001 Aug 24;276(34):31913-8. Epub 2001 Jun 4. PMID:11390410
Page seeded by OCA on Tue Nov 20 18:19:27 2007
