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Chembiochem

Title:		Peptoid-Peptide Hybrid Analogs of the Enterococcus faecalis Fsr Auto-Inducing Peptide (AIP) Reveal Crucial Structure-Activity Relationships
Author(s):		McBrayer DN; Ghosh U; Lella M; Cameron CD; Tal-Gan Y;
Address:		"Department of Chemistry, University of Nevada, Reno, 1664 N. Virginia Street, Reno, NV-89557, USA"
Journal Title:		Chembiochem
Year:		2023
Volume:		20221130
Issue:		1
Page Number:		e202200527 -
DOI:		10.1002/cbic.202200527
ISSN/ISBN:		1439-7633 (Electronic) 1439-4227 (Print) 1439-4227 (Linking)
Abstract:		"As multidrug-resistant bacteria become a more pressing risk to human health, alternate approaches to treating bacterial infections are being increasingly investigated. Enterococcus faecalis is an opportunistic pathogen responsible for a large percentage of secondary enterococci infections. Its pathogenicity has been shown to be largely dependent on a cell-density communication mechanism, termed quorum sensing. In this study, we conducted a systematic investigation of the lactone-containing macrocyclic signaling peptide used by E. faecalis for Fsr-mediated communication, termed gelatinase biosynthesis activating pheromone (GBAP). Specifically, through a combination of the on-resin sub-monomer and solution phase peptoid building block synthesis approaches, we successfully synthesized a library of peptoid-peptide hybrid analogs of GBAP and determined the biological effects associated with the introduction of the peptoid (N-alkyl glycine derivative) modifications. Within the macrocycle region of the peptide, as have been seen with other modifications, the F7 site was unusually tolerant toward peptoid modification, compared with other macrocyclic sites. Interestingly, within the exocyclic tail, peptoid modification at the N2 site completely abolished activity, a first for a single tail modification"
Keywords:		Humans *Enterococcus faecalis *Peptoids/pharmacology Bacterial Proteins/pharmacology Peptides/pharmacology Structure-Activity Relationship Enterococcus faecalis gelatinase biosynthesis activating pheromones peptidomimetics quorum sensing structure-activit;
Notes:		"MedlineMcBrayer, Dominic N Ghosh, Uttam Lella, Muralikrishna Cameron, Crissey D Tal-Gan, Yftah eng R35 GM128651/GM/NIGMS NIH HHS/ Research Support, N.I.H., Extramural Germany 2022/11/15 Chembiochem. 2023 Jan 3; 24(1):e202200527. doi: 10.1002/cbic.202200527. Epub 2022 Nov 30"