CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

Drugs therapeutic efficacy relies on their capability of binding the relevant targets in a physiological environment, which has so far been hard to measure. Here, the authors present a compound library screen based on a target engagement assay that reports on protein stability upon ligands binding i...

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Autores principales:	Helena Almqvist, Hanna Axelsson, Rozbeh Jafari, Chen Dan, André Mateus, Martin Haraldsson, Andreas Larsson, Daniel Martinez Molina, Per Artursson, Thomas Lundbäck, Pär Nordlund
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2016
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/07cf88c839fd460490c598e8b7898ec9
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spelling	oai:doaj.org-article:07cf88c839fd460490c598e8b7898ec92021-12-02T14:39:53ZCETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil10.1038/ncomms110402041-1723https://doaj.org/article/07cf88c839fd460490c598e8b7898ec92016-03-01T00:00:00Zhttps://doi.org/10.1038/ncomms11040https://doaj.org/toc/2041-1723Drugs therapeutic efficacy relies on their capability of binding the relevant targets in a physiological environment, which has so far been hard to measure. Here, the authors present a compound library screen based on a target engagement assay that reports on protein stability upon ligands binding in cell.Helena AlmqvistHanna AxelssonRozbeh JafariChen DanAndré MateusMartin HaraldssonAndreas LarssonDaniel Martinez MolinaPer ArturssonThomas LundbäckPär NordlundNature PortfolioarticleScienceQENNature Communications, Vol 7, Iss 1, Pp 1-11 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Helena Almqvist Hanna Axelsson Rozbeh Jafari Chen Dan André Mateus Martin Haraldsson Andreas Larsson Daniel Martinez Molina Per Artursson Thomas Lundbäck Pär Nordlund CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
description	Drugs therapeutic efficacy relies on their capability of binding the relevant targets in a physiological environment, which has so far been hard to measure. Here, the authors present a compound library screen based on a target engagement assay that reports on protein stability upon ligands binding in cell.
format	article
author	Helena Almqvist Hanna Axelsson Rozbeh Jafari Chen Dan André Mateus Martin Haraldsson Andreas Larsson Daniel Martinez Molina Per Artursson Thomas Lundbäck Pär Nordlund
author_facet	Helena Almqvist Hanna Axelsson Rozbeh Jafari Chen Dan André Mateus Martin Haraldsson Andreas Larsson Daniel Martinez Molina Per Artursson Thomas Lundbäck Pär Nordlund
author_sort	Helena Almqvist
title	CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
title_short	CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
title_full	CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
title_fullStr	CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
title_full_unstemmed	CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
title_sort	cetsa screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
publisher	Nature Portfolio
publishDate	2016
url	https://doaj.org/article/07cf88c839fd460490c598e8b7898ec9
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CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

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