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La inhibición de una beta-lactamasa de clase C por un monoester de fosfonato específico
1Chemistry Department, Wesleyan University, Middletown, CT 06457.
Science (New York, N.Y.)
|November 17, 1989
Resumen
Un nuevo monoester de fosfonato inhibe específicamente la beta-lactamasa de clase C de Enterobacter cloacae P99. Este descubrimiento puede conducir a nuevos antibióticos y inhibidores de la beta-lactamasa.
Área de la Ciencia:
- La bioquímica es la bioquímica.
- Microbiología Microbiología.
- Química Medicinal La Química Medicinal es un campo de estudio de la química medicinal.
Sus antecedentes:
- Las beta-lactamasas son enzimas que confieren resistencia bacteriana a los antibióticos beta-lactámicos.
- Las beta-lactamasas de clase C son un grupo significativo de estas enzimas de resistencia.
- El Enterobacter cloacae P99 produce una beta-lactamasa de clase C.
Objetivo del estudio:
- Para identificar inhibidores específicos de la clase C beta-lactamasa.
- Para investigar el mecanismo de inhibición por los monoesters de fosfonato.
Principales métodos:
- Los ensayos de cinética enzimática determinan las tasas de inhibición.
- Caracterización de la inactivación y reactivación de enzimas.
- Análisis espectroscópico para identificar sitios de modificación.
Principales resultados:
- El m-carboxifenil fenilacetamidometilfosfonato rápidamente inactiva el Enterobacter cloacae P99 clase C beta-lactamasas.
- La inactivación implica la fosforilación de un residuo en el sitio activo, liberando m-hidroxibenzoato.
- La reactivación enzimática es muy lenta, pero puede ser acelerada por nucleófilos específicos.
Conclusiones:
- Los monoésteres fosfonatos son potentes inhibidores específicos de la beta-lactamasa de clase C.
- El mecanismo implica una modificación covalente del sitio activo.
- Esta clase de compuestos muestra potencial para el desarrollo de nuevos antibióticos e inhibidores de la beta-lactamasa.
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