New inhibitors targeting bacterial RNA polymerase / 浙江大学学报·医学版
Journal of Zhejiang University. Medical sciences
;
(6): 44-49, 2019.
Artículo
en Chino
| WPRIM
| ID: wpr-775255
ABSTRACT
Rifamycins, a group of bacterial RNA polymerase inhibitors, are the firstline antimicrobial drugs to treat tuberculosis. In light of the emergence of rifamycinresistant bacteria, development of new RNA polymerase inhibitors that kill rifamycinresistant bacteria with high bioavailability is urgent. Structural analysis of bacterial RNA polymerase in complex with inhibitors by crystallography and cryo-EM indicates that RNA polymerase inhibitors function through five distinct molecular mechanismsinhibition of the extension of short RNA; competition with substrates; inhibition of the conformational change of the'bridge helix'; inhibition of clamp opening;inhibition of clamp closure. This article reviews the research progress of these five groups of RNA polymerase inhibitors to provide references for the modification of existing RNA polymerase inhibitors and the discovery of new RNA polymerase inhibitors.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Bacterias
/
Tuberculosis
/
ARN Polimerasas Dirigidas por ADN
/
ARN Bacteriano
/
Farmacorresistencia Bacteriana
/
Usos Terapéuticos
/
Quimioterapia
/
Activación Enzimática
/
Inhibidores Enzimáticos
Límite:
Humanos
Idioma:
Chino
Revista:
Journal of Zhejiang University. Medical sciences
Año:
2019
Tipo del documento:
Artículo
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