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Laboratory Variants GESG170L, GESG170K, and GESG170H Increase Carbapenem Hydrolysis and Confer Resistance to Clavulanic Acid.
Piccirilli, Alessandra; Mercuri, Paola Sandra; Segatore, Bernardetta; Galleni, Moreno; Brisdelli, Fabrizia; Kerff, Frédéric; Amicosante, Gianfranco; Perilli, Mariagrazia.
Affiliation
  • Piccirilli A; Dipartimento di Scienze Cliniche Applicate e Biotecnologiche, Università degli Studi dell'Aquila, L'Aquila, Italy alessandra.piccirilli@univaq.it mariagrazia.perilli@univaq.it.
  • Mercuri PS; Macromolécules Biologiques and Centre d'Ingénierie des Protéines, InBioS, Université de Liège, Liège, Belgium.
  • Segatore B; Dipartimento di Scienze Cliniche Applicate e Biotecnologiche, Università degli Studi dell'Aquila, L'Aquila, Italy.
  • Galleni M; Macromolécules Biologiques and Centre d'Ingénierie des Protéines, InBioS, Université de Liège, Liège, Belgium.
  • Brisdelli F; Dipartimento di Scienze Cliniche Applicate e Biotecnologiche, Università degli Studi dell'Aquila, L'Aquila, Italy.
  • Kerff F; Cristallographie des Macromolécules Biologiques, Centre d'Ingénierie des Protéines, InBioS, Université de Liège, Liège, Belgium.
  • Amicosante G; Dipartimento di Scienze Cliniche Applicate e Biotecnologiche, Università degli Studi dell'Aquila, L'Aquila, Italy.
  • Perilli M; Dipartimento di Scienze Cliniche Applicate e Biotecnologiche, Università degli Studi dell'Aquila, L'Aquila, Italy alessandra.piccirilli@univaq.it mariagrazia.perilli@univaq.it.
Antimicrob Agents Chemother ; 65(6)2021 05 18.
Article in En | MEDLINE | ID: mdl-33722888
ABSTRACT
The Guiana extended-spectrum (GES) ß-lactamase GESG170H, GESG170L, and GESG170K mutants showed kcat, Km , and kcat/Km values very dissimilar to those of GES-1 and GES-5. The enhancement of the hydrolytic activity against carbapenems is potentially due to a shift of the substrate in the active site that provides better positioning of the deacylating water molecule caused by the presence of the imidazole ring of H170 and of the long side chain of K170 and L170.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Carbapenems / Laboratories Language: En Journal: Antimicrob Agents Chemother Year: 2021 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Carbapenems / Laboratories Language: En Journal: Antimicrob Agents Chemother Year: 2021 Document type: Article