Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos SCIE SCOPUS

Cited 57 time in WEB OF SCIENCE Cited 64 time in Scopus
Title
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos
Author(s)
Jang, Kyoung Hwa; Chung, Soon-Chun; Shin, Jongheon; Lee, So-Hyoung; Kim, Tae-Im; Lee, Hyi-Seung; Oh, Ki-Bong
KIOST Author(s)
Lee, Hyi Seung(이희승)
Publication Year
2007-10-01
Abstract
Four aaptamines (1-4), 1H-benzo[de][1,6]-naphthyridine alkaloids, were isolated from the marine sponge Aoptos aaptos and their inhibitory activities against sortase A (SrtA), an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus, were evaluated. Isoaaptamine (2) was a potent inhibitor of SrtA, with an IC50 value of 3.7 +/- 0.2 mu g/mL. The suppression of fibronectin-binding activity by isoaaptamine (2) highlights its potential for the treatment of S. aureus infections via inhibition of SrtA activity. Our studies have identified a series of SrtA inhibitors, providing the basis for further development of potent inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.
ISSN
0960-894X
URI
https://sciwatch.kiost.ac.kr/handle/2020.kiost/4630
DOI
10.1016/j.bmcl.2007.08.007
Bibliographic Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.19, pp.5366 - 5369, 2007
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Subject
STAPHYLOCOCCUS-AUREUS SORTASE; SURFACE-PROTEINS; CELL-WALL; ANTINEOPLASTIC AGENTS; TRANSPEPTIDASE; ISOAAPTAMINE; PATHOGENESIS; CONVERSION; VIRULENCE; ENVELOPE
Keywords
aaptamines; sponge; Aaptos aaptos; Staphylococcus aureus; sortase A inhibition
Type
Article
Language
English
Document Type
Article
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
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