PMID:16251288
| Citation |
Baum, EZ, Crespo-Carbone, SM, Foleno, B, Peng, S, Hilliard, JJ, Abbanat, D, Goldschmidt, R and Bush, K (2005) Identification of a dithiazoline inhibitor of Escherichia coli L,D-carboxypeptidase A. Antimicrob. Agents Chemother. 49:4500-7 |
|---|---|
| Abstract |
The enzyme L,D-carboxypeptidase A is involved in the recycling of bacterial peptidoglycan and is essential in Escherichia coli during stationary phase. By high-throughput screening, we have identified a dithiazoline inhibitor of the enzyme with a 50% inhibitory concentration of 3 microM. The inhibitor appeared to cause lysis of E. coli during stationary phase, behavior that is similar to a previously described deletion mutant of L,D-carboxypeptidase A (M. F. Templin, A. Ursinus, and J.-V. Holtje, EMBO J. 18:4108-4117, 1999). As much as a one-log drop in CFU in stationary phase was observed upon treatment of E. coli with the inhibitor, and the amount of intracellular tetrapeptide substrate increased by approximately 33%, consistent with inhibition of the enzyme within bacterial cells. Stationary-phase targets such as L,D-carboxypeptidase A are largely underrepresented as targets of the antibiotic armamentarium but provide potential opportunities to interfere with bacterial growth and persistence. |
| Links |
PubMed PMC1280138 Online version:10.1128/AAC.49.11.4500-4507.2005 |
| Keywords |
Anti-Bacterial Agents/pharmacology; Carboxypeptidases A/antagonists & inhibitors; Enterobacteriaceae/drug effects; Escherichia coli/drug effects; Escherichia coli/enzymology; Protease Inhibitors/pharmacology; Substrate Specificity; Thiazoles/pharmacology |
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