Ontology highlight
ABSTRACT:
SUBMITTER: Wang J
PROVIDER: S-EPMC5817083 | biostudies-literature | 2018
REPOSITORIES: biostudies-literature
Wang Jianfeng J Li Hongen H Pan Juan J Dong Jing J Zhou Xuan X Niu Xiaodi X Deng Xuming X
Frontiers in microbiology 20180214
Sortase A (SrtA)-catalyzed anchorage of surface proteins in most Gram-positive bacteria is indispensable for their virulence, suggesting that this transpeptidase is a promising target for antivirulence therapy. Here, an oligopeptide, LPRDA, was identified as an effective inhibitor of SrtA via virtual screening based on the LPXTG substrate sequence, and it was found to inhibit SrtA activity <i>in vitro</i> and <i>in vivo</i> (IC<sub>50</sub> = 10.61 μM) by competitively occupying the active site ...[more]