The Triphenylethylenes, a Novel Class of Antifungals

ABSTRACT New antifungals are needed, particularly in the developing world, to treat life-threatening fungal infections, such as cryptococcosis. Drug repurposing is one strategy to identify new drug-like compounds, but it is often difficult to identify a mechanism of action. Here we discuss the outst...

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Autor principal:	Audrey R. Odom
Formato:	article
Lenguaje:	EN
Publicado:	American Society for Microbiology 2014
Materias:	Microbiology QR1-502
Acceso en línea:	https://doaj.org/article/093d3bb8f257490292a0d2530c6d76c8
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spelling	oai:doaj.org-article:093d3bb8f257490292a0d2530c6d76c82021-11-15T15:47:39ZThe Triphenylethylenes, a Novel Class of Antifungals10.1128/mBio.01126-142150-7511https://doaj.org/article/093d3bb8f257490292a0d2530c6d76c82014-07-01T00:00:00Zhttps://journals.asm.org/doi/10.1128/mBio.01126-14https://doaj.org/toc/2150-7511ABSTRACT New antifungals are needed, particularly in the developing world, to treat life-threatening fungal infections, such as cryptococcosis. Drug repurposing is one strategy to identify new drug-like compounds, but it is often difficult to identify a mechanism of action. Here we discuss the outstanding effort by Butts et al. to identify calmodulin as an antifungal target of repurposed estrogen receptor antagonists [A. Butts, K. Koselny, Y. Chabrier-Roselló, C. P. Semighini, Y. C. S. Brown, et al., mBio 5(1):e00765-13, 2014, doi:10.1128/mBio.00765-13]. The authors show that these compounds bind to and directly inhibit fungal calmodulin and also reduce fungal burden in an animal disease model. These studies thus establish both the key preclinical efficacy and the antifungal mechanism of action, which will allow these compounds to progress toward development of novel antifungal therapies.Audrey R. OdomAmerican Society for MicrobiologyarticleMicrobiologyQR1-502ENmBio, Vol 5, Iss 3 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Microbiology QR1-502
spellingShingle	Microbiology QR1-502 Audrey R. Odom The Triphenylethylenes, a Novel Class of Antifungals
description	ABSTRACT New antifungals are needed, particularly in the developing world, to treat life-threatening fungal infections, such as cryptococcosis. Drug repurposing is one strategy to identify new drug-like compounds, but it is often difficult to identify a mechanism of action. Here we discuss the outstanding effort by Butts et al. to identify calmodulin as an antifungal target of repurposed estrogen receptor antagonists [A. Butts, K. Koselny, Y. Chabrier-Roselló, C. P. Semighini, Y. C. S. Brown, et al., mBio 5(1):e00765-13, 2014, doi:10.1128/mBio.00765-13]. The authors show that these compounds bind to and directly inhibit fungal calmodulin and also reduce fungal burden in an animal disease model. These studies thus establish both the key preclinical efficacy and the antifungal mechanism of action, which will allow these compounds to progress toward development of novel antifungal therapies.
format	article
author	Audrey R. Odom
author_facet	Audrey R. Odom
author_sort	Audrey R. Odom
title	The Triphenylethylenes, a Novel Class of Antifungals
title_short	The Triphenylethylenes, a Novel Class of Antifungals
title_full	The Triphenylethylenes, a Novel Class of Antifungals
title_fullStr	The Triphenylethylenes, a Novel Class of Antifungals
title_full_unstemmed	The Triphenylethylenes, a Novel Class of Antifungals
title_sort	triphenylethylenes, a novel class of antifungals
publisher	American Society for Microbiology
publishDate	2014
url	https://doaj.org/article/093d3bb8f257490292a0d2530c6d76c8
work_keys_str_mv	AT audreyrodom thetriphenylethylenesanovelclassofantifungals AT audreyrodom triphenylethylenesanovelclassofantifungals
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The Triphenylethylenes, a Novel Class of Antifungals

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