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La "región de conmutación" de la ARN polimerasa es un objetivo para los inhibidores
Jayanta Mukhopadhyay1, Kalyan Das, Sajida Ismail
1Howard Hughes Medical Institute, Rutgers University, Piscataway, NJ 08854, USA.
Cell
|October 30, 2008
Resumen
El antibiótico Myxopyronin inhibe la ARN polimerasa bacteriana (RNAP) al dirigirse a la región del interruptor, evitando la unión al ADN. Este mecanismo ofrece una nueva vía para el desarrollo de fármacos antibacterianos de amplio espectro.
Área de la Ciencia:
- Microbiología Microbiología.
- Biología Molecular Biología Molecular
- Descubrimiento de Drogas Descubrimiento de Drogas
Sus antecedentes:
- La ARN polimerasa bacteriana (ARNP) es un objetivo crucial para los antibióticos.
- Los inhibidores de RNAP existentes se dirigen a sitios distintos de la región de conmutación.
Objetivo del estudio:
- Para dilucidar el mecanismo de acción de la mixopironina (Myx) en el RNAP. bacteriano.
- Investigar el potencial de la región de conmutación de RNAP como objetivo para nuevos antibióticos.
Principales métodos:
- El análisis genético.
- Pruebas bioquímicas de ensayos.
- Estudios estructurales (por ejemplo, cristalografía de rayos X)
- Perfilado de la resistencia a los antibióticos.
Principales resultados:
- Myx se une a la región de conmutación de RNAP, inhibiendo la interacción de RNAP-promotor de ADN.
- Myx previene la apertura de la hendidura del centro activo de RNAP necesaria para el inicio de la transcripción.
- Los antibióticos estructuralmente relacionados (corallopironina) y no relacionados (ripostatina) comparten este mecanismo inhibidor.
- Myx, corallopironina y ripostatina no muestran resistencia cruzada con los inhibidores de la RNAP existentes.
Conclusiones:
- La región de conmutación de RNAP es un nuevo objetivo para los agentes antibacterianos.
- La mixopironina y sus compuestos relacionados representan una nueva clase de inhibidores de la RNAP.
- Dirigirse a la región de cambio ofrece potencial para el desarrollo de antibióticos de amplio espectro con nuevos mecanismos de acción.
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