US 12,662,513 B2 · Peptidic modulators of quorum sensing in Staphylococcus epidermidis

Abstract

Synthetic cyclic peptide modulators of the AgrC quorum sensing system of S. epidermidis. Synthetic agonists and antagonist of AgrC-I are described. Compounds capable of either pan-group or group-selective AgrC receptor inhibition in S. epidermidis were identified. Additionally, compounds that are species selective, and could be applied to selectively modulate either S. epidermidis or S. aureus AgrC receptors were identified. An AgrC-I agonist was found which strongly inhibits S. epidermidis biofilm growth, with a higher potency and efficacy than that of native AIP-I. Methods of modulating virulence in S. epidermidis and related Staphylococcus by contacting a bacterium or a bacterial environment, such as a biofilm, with a modulator of the disclosure are provided. Methods are provided for treating infections of S. epidermidis and related Staphylococcus by administering a therapeutically effective amount of one or more compounds herein to an individual in need thereof.

Claims5

Dependent claims

A compound which is selected from the peptides of:

(SEQ ID NO:
176)
K-Y-L-P-(C-S-N-Y-L),
(SEQ ID NO:
177)
K-Y-V-P-(C-S-N-Y-L),
(SEQ ID NO:
178)
K-Y-N-V-(C-S-N-Y-L),
(SEQ ID NO:
179)
K-Y-N-V-(C-A-N-Y-L),
(SEQ ID NO:
180)
K-Y-N-V-(C-S-A-Y-L),
(SEQ ID NO:
181)
K-Y-N-V-(C-S-S-Y-L),
(SEQ ID NO:
94)
A-S-A-(C-A-A-Y-F),
(SEQ ID NO:
95)
A-S-A-(C-S-A-Y-F)
or salts of any thereof.

22 more elements

Dependencies are inferred from the claim text.

Facts

Application

16/098,394Filed 1 May 2017 · us provisional application

Priority

1 May 2016

Published

US 2020/0308230 A11 Oct 2020

Granted

23 Jun 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

C07K 7/64
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof: cyclic peptides containing only normal peptide links
A61P 31/04
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antibacterial agents
C07K 7/56
With at least one abnormal peptide link in the ring: the cyclisation not occurring through 2,4-diamino-butanoic acid
A61K 38/00
Medicinal preparations containing peptides

Peptidic modulators of quorum sensing in Staphylococcus epidermidis

Life of this patent

Peptidic modulators of quorum sensing in Staphylococcus epidermidis

Life of this patent

Abstract

Claims5