Simple Strategy for Taming Membrane-Disrupting Antibiotics

[Image: see text] 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 t...

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Autores principales: Yu, Yuming, Sabulski, Mary J., Schell, Wiley A., Pires, Marcos M., Perfect, John R., Regen, Steven L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5184371/
https://www.ncbi.nlm.nih.gov/pubmed/27801580
http://dx.doi.org/10.1021/acs.bioconjchem.6b00629
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author Yu, Yuming
Sabulski, Mary J.
Schell, Wiley A.
Pires, Marcos M.
Perfect, John R.
Regen, Steven L.
author_facet Yu, Yuming
Sabulski, Mary J.
Schell, Wiley A.
Pires, Marcos M.
Perfect, John R.
Regen, Steven L.
author_sort Yu, Yuming
collection PubMed
description [Image: see text] 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.
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spelling pubmed-51843712016-12-27 Simple Strategy for Taming Membrane-Disrupting Antibiotics Yu, Yuming Sabulski, Mary J. Schell, Wiley A. Pires, Marcos M. Perfect, John R. Regen, Steven L. Bioconjug Chem [Image: see text] 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. American Chemical Society 2016-11-01 2016-12-21 /pmc/articles/PMC5184371/ /pubmed/27801580 http://dx.doi.org/10.1021/acs.bioconjchem.6b00629 Text en Copyright © 2016 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Yu, Yuming
Sabulski, Mary J.
Schell, Wiley A.
Pires, Marcos M.
Perfect, John R.
Regen, Steven L.
Simple Strategy for Taming Membrane-Disrupting Antibiotics
title Simple Strategy for Taming Membrane-Disrupting Antibiotics
title_full Simple Strategy for Taming Membrane-Disrupting Antibiotics
title_fullStr Simple Strategy for Taming Membrane-Disrupting Antibiotics
title_full_unstemmed Simple Strategy for Taming Membrane-Disrupting Antibiotics
title_short Simple Strategy for Taming Membrane-Disrupting Antibiotics
title_sort simple strategy for taming membrane-disrupting antibiotics
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5184371/
https://www.ncbi.nlm.nih.gov/pubmed/27801580
http://dx.doi.org/10.1021/acs.bioconjchem.6b00629
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