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BioAssay: AID 575012

Activity of Pseudomonas aeruginosa beta-lactamase IMP-1 by UV spectrophotometric analysis

ME1071, a maleic acid derivative, is a novel specific inhibitor for metallo-beta-lactamases (MBL). In this study, the potentiation of ME1071 in combination with several beta-lactams was evaluated using MBL-producing Pseudomonas aeruginosa isolates. The rates of susceptibility of MBL producers to carbapenems (imipenem, biapenem, and doripenem) and ceftazidime were increased by 8 to 27% in the more ..
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(1)
 
 
Inconclusive(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(1)
 
 
Inconclusive(1)
 
 
Unspecified(1)
 
 
AID: 575012
Data Source: ChEMBL (723552)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2014-05-27

Data Table ( Complete ):           Active    All
Target
Sequence: Metallo-beta-lactamase IMP-1 (Beta-lactamase IMP-1) (Metallo-beta-lactamase) (IMP-1 metallo-beta-lactmase) (Beta-lactamase) (Extended-spectrum B-lactamase) (Bla-imp protein)
Description ..   
Comment ..   

     More BioActivity Data..
BioActive Compound: 1
Description:
Title: In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.

Abstract: ME1071, a maleic acid derivative, is a novel specific inhibitor for metallo-beta-lactamases (MBL). In this study, the potentiation of ME1071 in combination with several beta-lactams was evaluated using MBL-producing Pseudomonas aeruginosa isolates. The rates of susceptibility of MBL producers to carbapenems (imipenem, biapenem, and doripenem) and ceftazidime were increased by 8 to 27% in the presence of 32 microg/ml of ME1071. The corresponding resistance rates were decreased by 13 to 46%, respectively. On the other hand, ME1071 showed weaker or no potentiation with non-MBL producers. The K(i) value of ME1071 for IMP-1 was 0.4 microM, significantly lower than the K(m) values of carbapenems for the IMP-1 enzyme. On the other hand, the K(i) value of ME1071 for VIM-2 was 120 microM, higher than the K(m) values of carbapenems for the VIM-2 enzyme. Results of this study indicate that ME1071 can potentiate the activity of ceftazidime and carbapenems against MBL-producing strains of P. aeruginosa.
(PMID: 20606062)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Km*Km PubChem standard valueFloatμM
2Kcat activity commentKcat activity commentString
3Kcat standard flagKcat standard flagInteger
4Kcat qualifierKcat qualifierString
5Kcat published valueKcat published valueFloat/s
6Kcat standard valueKcat standard valueFloats-1
7Km activity commentKm activity commentString
8Km standard flagKm standard flagInteger
9Km qualifierKm qualifierString
10Km published valueKm published valueFloatμM
11Km standard valueKm standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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