Simple Strategy for Taming Membrane-Disrupting Antibiotics.

Journal Article

A strategy has been devised for increasing the cellular selectivity of membrane-disrupting antibiotics based on the attachment of a facially amphiphilic sterol. Using Amphotericin B (AmB) as a prototype, covalent attachment of cholic acid bound to a series of α,ω-diamines has led to a dramatic reduction in hemolytic activity, a significant reduction in toxicity toward HEK293T cells, and significant retention of antifungal activity.

Full Text

Duke Authors

Cited Authors

  • Yu, Y; Sabulski, MJ; Schell, WA; Pires, MM; Perfect, JR; Regen, SL

Published Date

  • December 2016

Published In

Volume / Issue

  • 27 / 12

Start / End Page

  • 2850 - 2853

PubMed ID

  • 27801580

Electronic International Standard Serial Number (EISSN)

  • 1520-4812

International Standard Serial Number (ISSN)

  • 1043-1802

Digital Object Identifier (DOI)

  • 10.1021/acs.bioconjchem.6b00629

Language

  • eng