Journal
BIOCONJUGATE CHEMISTRY
Volume 27, Issue 12, Pages 2850-2853Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.6b00629
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Funding
- National Institutes of Health [PHS GM100962]
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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 alpha,omega-diamines has led to a dramatic reduction in hemolytic activity, a significant reduction in toxicity toward HEK293T cells, and significant retention of antifungal activity.
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