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Estructura e inhibición de la tuberculosinol sintasa y la decaprenila difosfato sintasa de las bacterias
Hsiu-Chien Chan1, Xinxin Feng, Tzu-Ping Ko
1Industrial Enzymes National Engineering Laboratory, Tianjin Institute of Industrial Biotechnology , Tianjin 300308, China.
Journal of the American Chemical Society
|January 31, 2014
Resumen
Los investigadores aclararon la estructura de una enzima clave en Mycobacterium tuberculosis, Rv3378c, revelando su mecanismo único. Este descubrimiento puede conducir a nuevas terapias anti-infecciosas dirigidas a la virulencia bacteriana y la biosíntesis de la pared celular.
Área de la Ciencia:
- Biología estructural Biología estructural.
- La bioquímica es la bioquímica.
- Descubrimiento de fármacos.
Sus antecedentes:
- Mycobacterium tuberculosis es un patógeno que requiere nuevas estrategias anti-infecciosas.
- Las diterpenas sintasas bacterianas juegan un papel en la formación del factor de virulencia.
- Rv3378c es un objetivo potencial de fármaco para bloquear la virulencia.
Objetivo del estudio:
- Para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis. para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis. para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis. para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis. para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis. para determinar la estructura de Rv3378c, una diterpena sintasa bacteriana de Mycobacterium tuberculosis.
- Para aclarar el mecanismo de acción de Rv3378c.c.
- Proporcionar conocimientos estructurales para el desarrollo de nuevos agentes antiinfecciosos.
Principales métodos:
- Se utilizó la cristalografía de rayos X para obtener las estructuras de Rv3378c.
- Se determinaron las estructuras para la enzima sola, con sustrato y con un inhibidor.
- Se empleó la mutagenesis dirigida al sitio para investigar el mecanismo de la enzima.
Principales resultados:
- Se determinó la estructura de Rv3378c, revelando un pliegue similar al de las preniltransferasas.
- Las estructuras con sustrato e inhibidor proporcionaron información sobre los mecanismos de unión e inhibición.
- La evidencia sugiere un mecanismo catalítico inusual que involucra dos residuos de tirosina.
Conclusiones:
- Rv3378c comparte similitudes estructurales y funcionales con la M. tuberculosis cis-decaprenil difosfato sintasa (DPPS).
- Los datos estructurales y los conocimientos mecanicistas pueden guiar el desarrollo de inhibidores de doble acción.
- Estos inhibidores podrían dirigirse tanto a la virulencia bacteriana como a la biosíntesis de la pared celular.
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