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Titolo:
Inhibition of IMP-1 metallo-beta-lactamase and sensitization of TMP-1-producing bacteria by thioester derivatives
Autore:
Hammond, GG; Huber, JL; Greenlee, ML; Laub, JB; Young, K; Silver, LL; Balkovec, JM; Pryor, KD; Wu, JK; Leiting, B; Pompliano, DL; Toney, JH;
Indirizzi:
Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA Merck Res Labs Rahway NJ USA 07065 bs, Dept Biochem, Rahway, NJ 07065 USA Merck Res Labs, Dept Infect Dis Res, Rahway, NJ 07065 USA Merck Res Labs Rahway NJ USA 07065 t Infect Dis Res, Rahway, NJ 07065 USA Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA Merck Res Labs RahwayNJ USA 07065 s, Dept Med Chem, Rahway, NJ 07065 USA
Titolo Testata:
FEMS MICROBIOLOGY LETTERS
fascicolo: 2, volume: 179, anno: 1999,
pagine: 289 - 296
SICI:
0378-1097(19991015)179:2<289:IOIMAS>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
THIOL ESTER DERIVATIVES; BACTEROIDES-FRAGILIS; SERRATIA-MARCESCENS; IMIPENEM RESISTANCE; CRYSTAL-STRUCTURE; EXPRESSION; RESOLUTION; SERIES; ACID;
Keywords:
metallo-beta-lactamase; thioester; IMP-1;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Toney, JH Merck Res Labs, Dept Biochem, POB 2000, Rahway, NJ 07065 USA Merck Res Labs POB 2000 Rahway NJ USA 07065 Rahway, NJ 07065 USA
Citazione:
G.G. Hammond et al., "Inhibition of IMP-1 metallo-beta-lactamase and sensitization of TMP-1-producing bacteria by thioester derivatives", FEMS MICROB, 179(2), 1999, pp. 289-296

Abstract

IMP-1 metallo-beta-lactamase is a transferable carbapenem-hydrolyzing enzyme found in some clinical isolates of Pseudomonas aeruginosa, Serratia marcescens and Klebsiella pneumoniae. Bacteria that express IMP-1 show significantly reduced sensitivity to carbapenems and other beta-lactam antibiotics. A series of thioester derivatives has been shown to competitively inhibit purified IMP-1. As substrates for IMP-1, the thioesters yielded thiol hydrolysis products which themselves were reversible competitive inhibitors. Thethioesters also increased sensitivity to the carbapenem L-742,728 in an IMP-1-producing laboratory stain of Escherichia coli, but will need further modification to improve their activity in less permeable organisms such as Pseudomonas and Serratia. Nonetheless, the thioester IMP-1 inhibitors offer an encouraging start to overcoming merallo-beta-lactamase-mediated resistance in bacteria. (C) 1994 Federation of European Microbiological Societies. Published by Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 20:29:32