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Simple Strategy for Taming Membrane-Disrupting Antibiotics

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journal contribution
posted on 01.11.2016, 00:00 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.