creators_name: Lohan, Sandeep
creators_name: Kalanta, Arneesh
creators_name: Sonkusre, Praveen
creators_name: Cameotra, Swaranjit Singh
creators_name: Bisht, Gopal Singh
type: article
datestamp: 2015-02-10 04:30:25
lastmod: 2015-02-10 04:30:25
metadata_visibility: show
title: Development of novel membrane active lipidated peptidomimetics active against drug resistant clinical isolates.
ispublished: pub
keywords: Antimicrobial peptides; Drug resistance; Lipopeptides; Membranolytic; Peptidomimetics
abstract: A new series of small cationic lipidated peptidomimetics have been synthesized and found to be highly active against several susceptible as well as drug resistant clinical isolates of bacteria and fungi. All lipidated peptidomimetics do not cause significant lysis of human erythrocytes (HC50>200μg/mL). Calcein dye leakage experiment revealed membranolytic effect of LPEP08 which was further confirmed by scanning electron microscopy (SEM). The involvement of intracellular targets as an alternate mode of action was precluded by DNA retardation assay. Additionally, LPEP08 exhibit high proteolytic stability and dose not elicit resistance against drug resistant clinical isolate of Staphylococcusaureus, even after 16 rounds of passaging. These results demonstrate the potential of lipidated peptidomimetics as biocompatible anti-infective therapeutics.
date: 2014-09-01
date_type: published
publication: Bioorganic & medicinal chemistry
volume: 22
number: 17
publisher: Oxford : Elsevier Science
pagerange: 4544-52
refereed: TRUE
issn: 1464-3391
official_url: http://www.sciencedirect.com/science/article/pii/S0968089614005574
citation:   Lohan, Sandeep and Kalanta, Arneesh and Sonkusre, Praveen and Cameotra, Swaranjit Singh and Bisht, Gopal Singh  (2014) Development of novel membrane active lipidated peptidomimetics active against drug resistant clinical isolates.  Bioorganic & medicinal chemistry, 22 (17).  pp. 4544-52.  ISSN 1464-3391