Novel inhibitors against the bacterial signal peptidase I / 药学学报
Acta Pharmaceutica Sinica
; (12): 1561-6, 2012.
Article
in Zh
| WPRIM
| ID: wpr-433014
Responsible library:
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.
Full text:
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Index:
WPRIM
Type of study:
Prognostic_studies
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article