bc6b00629_si_001.pdf (7.01 MB)
Simple Strategy for Taming Membrane-Disrupting Antibiotics
journal contribution
posted on 2016-11-01, 00:00 authored by Yuming Yu, Mary J. Sabulski, Wiley
A. Schell, Marcos M. Pires, John R. Perfect, Steven L. RegenA 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.