Linear peptidomimetics as potent antagonists of Staphylococcus aureus agr quorum sensing
Research output: Contribution to journal › Journal article › peer-review
Standard
Linear peptidomimetics as potent antagonists of Staphylococcus aureus agr quorum sensing. / Karathanasi, Georgia; Bojer, Martin Saxtorph; Baldry, Mara; Johannessen, Bárdur Andréson; Wolff, Sanne; Greco, Ines; Kilstrup, Mogens; Hansen, Paul Robert; Ingmer, Hanne.
In: Scientific Reports, Vol. 8, No. 1, 3562, 2018.Research output: Contribution to journal › Journal article › peer-review
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Linear peptidomimetics as potent antagonists of Staphylococcus aureus agr quorum sensing
AU - Karathanasi, Georgia
AU - Bojer, Martin Saxtorph
AU - Baldry, Mara
AU - Johannessen, Bárdur Andréson
AU - Wolff, Sanne
AU - Greco, Ines
AU - Kilstrup, Mogens
AU - Hansen, Paul Robert
AU - Ingmer, Hanne
PY - 2018
Y1 - 2018
N2 - Staphylococcus aureus is an important pathogen causing infections in humans and animals. Increasing problems with antimicrobial resistance has prompted the development of alternative treatment strategies, including antivirulence approaches targeting virulence regulation such as the agr quorum sensing system. agr is naturally induced by cyclic auto-inducing peptides (AIPs) binding to the AgrC receptor and cyclic peptide inhibitors have been identified competing with AIP binding to AgrC. Here, we disclose that small, linear peptidomimetics can act as specific and potent inhibitors of the S. aureus agr system via intercepting AIP-AgrC signal interaction at low micromolar concentrations. The corresponding linear peptide did not have this ability. This is the first report of a linear peptide-like molecule that interferes with agr activation by competitive binding to AgrC. Prospectively, these peptidomimetics may be valuable starting scaffolds for the development of new inhibitors of staphylococcal quorum sensing and virulence gene expression.
AB - Staphylococcus aureus is an important pathogen causing infections in humans and animals. Increasing problems with antimicrobial resistance has prompted the development of alternative treatment strategies, including antivirulence approaches targeting virulence regulation such as the agr quorum sensing system. agr is naturally induced by cyclic auto-inducing peptides (AIPs) binding to the AgrC receptor and cyclic peptide inhibitors have been identified competing with AIP binding to AgrC. Here, we disclose that small, linear peptidomimetics can act as specific and potent inhibitors of the S. aureus agr system via intercepting AIP-AgrC signal interaction at low micromolar concentrations. The corresponding linear peptide did not have this ability. This is the first report of a linear peptide-like molecule that interferes with agr activation by competitive binding to AgrC. Prospectively, these peptidomimetics may be valuable starting scaffolds for the development of new inhibitors of staphylococcal quorum sensing and virulence gene expression.
U2 - 10.1038/s41598-018-21951-4
DO - 10.1038/s41598-018-21951-4
M3 - Journal article
C2 - 29476092
VL - 8
JO - Scientific Reports
JF - Scientific Reports
SN - 2045-2322
IS - 1
M1 - 3562
ER -
ID: 191962949