Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions

Small molecule stabilizers of protein–protein interactions hold great therapeutic potential. Based on virtual screening and molecular docking, the authors here develop a strategy to evolve weak, promiscuous inhibitors of 14-3-3 interactions into selective stabilizers of the 14-3-3/ChREBP complex.

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Autores principales: Eline Sijbesma, Emira Visser, Kathrin Plitzko, Philipp Thiel, Lech-Gustav Milroy, Markus Kaiser, Luc Brunsveld, Christian Ottmann
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Lenguaje:EN
Publicado: Nature Portfolio 2020
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Acceso en línea:https://doaj.org/article/8ff8fc48608f42e5b0be3c2e5c15b283
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spelling oai:doaj.org-article:8ff8fc48608f42e5b0be3c2e5c15b2832021-12-02T18:49:31ZStructure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions10.1038/s41467-020-17741-02041-1723https://doaj.org/article/8ff8fc48608f42e5b0be3c2e5c15b2832020-08-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-17741-0https://doaj.org/toc/2041-1723Small molecule stabilizers of protein–protein interactions hold great therapeutic potential. Based on virtual screening and molecular docking, the authors here develop a strategy to evolve weak, promiscuous inhibitors of 14-3-3 interactions into selective stabilizers of the 14-3-3/ChREBP complex.Eline SijbesmaEmira VisserKathrin PlitzkoPhilipp ThielLech-Gustav MilroyMarkus KaiserLuc BrunsveldChristian OttmannNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-9 (2020)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Eline Sijbesma
Emira Visser
Kathrin Plitzko
Philipp Thiel
Lech-Gustav Milroy
Markus Kaiser
Luc Brunsveld
Christian Ottmann
Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
description Small molecule stabilizers of protein–protein interactions hold great therapeutic potential. Based on virtual screening and molecular docking, the authors here develop a strategy to evolve weak, promiscuous inhibitors of 14-3-3 interactions into selective stabilizers of the 14-3-3/ChREBP complex.
format article
author Eline Sijbesma
Emira Visser
Kathrin Plitzko
Philipp Thiel
Lech-Gustav Milroy
Markus Kaiser
Luc Brunsveld
Christian Ottmann
author_facet Eline Sijbesma
Emira Visser
Kathrin Plitzko
Philipp Thiel
Lech-Gustav Milroy
Markus Kaiser
Luc Brunsveld
Christian Ottmann
author_sort Eline Sijbesma
title Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
title_short Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
title_full Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
title_fullStr Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
title_full_unstemmed Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
title_sort structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
publisher Nature Portfolio
publishDate 2020
url https://doaj.org/article/8ff8fc48608f42e5b0be3c2e5c15b283
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