Novel inhibitors against the bacterial signal peptidase I / 药学学报
Acta Pharmaceutica Sinica
; (12): 1561-1566, 2012.
Article
em Zh
| WPRIM
| ID: wpr-274622
Biblioteca responsável:
WPRO
ABSTRACT
New antibiotics with novel modes of action and structures are urgently needed to combat the emergence of multidrug-resistant bacteria. Bacterial signal peptidase I (SPase I) is an indispensable enzyme responsible for cleaving the signal peptide of preprotein to release the matured proteins. Increasing evidence suggests that SPase I plays a crucial role in bacterial pathogenesis by regulating the excretion of a variety of virulent factors, maturation of quorum sensing factor and the intrinsic resistance against beta-lactams. Recently, breakthrough has been achieved in the understanding of three-dimensional structure of SPase I as well as the mechanism of enzyme-inhibitors interaction. Three families of inhibitors are identified, i.e. signal peptide derivatives, beta-lactams and arylomycins. In this article, we summarize the recent advance in the study of structure, activity and structure-activity relationship of SPase I inhibitors.
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Oligopeptídeos
/
Farmacologia
/
Relação Estrutura-Atividade
/
Bactérias
/
Serina Endopeptidases
/
Inibidores de Serina Proteinase
/
Química
/
Beta-Lactamas
/
Escherichia coli
/
Proteínas de Membrana
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Article