Novel inhibitors against the bacterial signal peptidase I / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1561-1566, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-274622
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:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Oligopeptides
/
Pharmacology
/
Structure-Activity Relationship
/
Bacteria
/
Serine Endopeptidases
/
Serine Proteinase Inhibitors
/
Chemistry
/
Beta-Lactams
/
Escherichia coli
/
Membrane Proteins
Type of study:
Prognostic study
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
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