figshare
Browse
bc6b00629_si_001.pdf (7.01 MB)

Simple Strategy for Taming Membrane-Disrupting Antibiotics

Download (7.01 MB)
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. Regen
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.

History