Simple Strategy for Taming Membrane-Disrupting Antibiotics.
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ABSTRACT:
SUBMITTER: Yu Y
PROVIDER: S-EPMC5184371 | biostudies-literature | 2016 Dec
REPOSITORIES: biostudies-literature
Publications
Simple Strategy for Taming Membrane-Disrupting Antibiotics.
Yu Yuming Y Sabulski Mary J MJ Schell Wiley A WA Pires Marcos M MM Perfect John R JR Regen Steven L SL
Bioconjugate chemistry 20161109 12
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. ...[more]
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