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.
Artigo
em Chinês
| 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:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Bactérias
/
Tuberculose
/
RNA Polimerases Dirigidas por DNA
/
RNA Bacteriano
/
Farmacorresistência Bacteriana
/
Usos Terapêuticos
/
Tratamento Farmacológico
/
Ativação Enzimática
/
Inibidores Enzimáticos
Limite:
Humanos
Idioma:
Chinês
Revista:
Journal of Zhejiang University. Medical sciences
Ano de publicação:
2019
Tipo de documento:
Artigo
Similares
MEDLINE
...
LILACS
LIS