Taming Amphotericin B

Bioconjugate Chemistry
Vaclav JanoutSteven L Regen

Abstract

A strategy is introduced for enhancing the cellular selectivity of Amphotericin B (AmB) and other classes of membrane-disrupting agents. This strategy involves attaching the agent to a molecular umbrella to minimize the disruptive power of aggregated forms. Based on this approach, AmB has been coupled to a molecular umbrella derived from one spermidine and two cholic acid molecules and found to have antifungal activities approaching that of the native drug. However, in sharp contrast to AmB, the hemolytic activity and the cytotoxcity of this conjugate toward HEK293 T cells have been dramatically reduced.

References

Nov 1, 1992·Antimicrobial Agents and Chemotherapy·P LegrandJ Bolard
Jul 19, 2008·Science·Brian C Monk, Andre Goffeau
Sep 12, 2008·Journal of the American Chemical Society·Masaharu KondoSteven L Regen
Dec 5, 2008·Bioconjugate Chemistry·Vaclav Janout, Steven L Regen
Nov 26, 2009·Mini Reviews in Medicinal Chemistry·Milos Sedlák
Jun 18, 2010·Natural Product Reports·Astrid A VolmerErick M Carreira
Jul 9, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Kun ShaoChen Jiang
Mar 4, 2011·Proceedings of the National Academy of Sciences of the United States of America·Daniel S PalaciosMartin D Burke
Feb 7, 2012·Proceedings of the National Academy of Sciences of the United States of America·Kaitlyn C GrayMartin D Burke
Dec 21, 2012·Science Translational Medicine·Gordon D BrownTheodore C White
May 30, 2013·Antimicrobial Agents and Chemotherapy·Anna N TevyashovaMaria N Preobrazhenskaya
May 31, 2013·Journal of the American Chemical Society·Brandon C WilcockMartin D Burke
Oct 9, 2013·Frontiers in Microbiology·Diana GasparMiguel A R B Castanho
Apr 1, 2014·Nature Chemical Biology·Thomas M AndersonMartin D Burke
May 21, 2015·Journal of the American Chemical Society·Pol Arranz-GibertErnest Giralt
Jun 2, 2015·Nature Chemical Biology·Stephen A DavisMartin D Burke
Jul 10, 2015·ACS Infectious Diseases·Mark A T BlaskovichMatthew A Cooper

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Citations

Dec 1, 2015·International Journal of Pharmaceutics·Cláudia SerafimLuis Garcia-Rio
Jun 25, 2016·Nanomedicine : Nanotechnology, Biology, and Medicine·Andrzej S SkwareckiMaria J Milewska
Apr 23, 2016·Expert Opinion on Drug Delivery·Célia FaustinoCatarina Pinto Reis
Nov 2, 2016·Bioconjugate Chemistry·Yuming YuSteven L Regen
May 13, 2017·Nature Reviews. Drug Discovery·John R Perfect
Feb 20, 2018·Applied Microbiology and Biotechnology·Lasse van GeelenRainer Kalscheuer
May 16, 2018·Annals of the New York Academy of Sciences·Jennifer Geddes-McAlister, Rebecca S Shapiro
Jul 7, 2016·Antimicrobial Agents and Chemotherapy·B Eleazar Cohen
Jan 8, 2020·Pharmaceutics·Célia Faustino, Lídia Pinheiro
Oct 2, 2016·Journal of Fungi·Kaila M Pianalto, J Andrew Alspaugh
Jan 17, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Steven L Regen
Feb 23, 2021·Royal Society Open Science·Thomas SwiftStephen Rimmer
Oct 30, 2020·The Journal of Physical Chemistry. B·Lais AlonsoAntonio Alonso
Feb 28, 2018·Bioconjugate Chemistry·Andrzej S SkwareckiSławomir Milewski

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