Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction

Directed protein degradation to target hard-to-drug proteins is a promising therapeutic approach. Here, the authors report the prospective discovery of small molecule “molecular glue” that inserts into a naturally occurring E3 ligase-substrate interface leading to degradation of substrate protein....

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Autores principales: Kyle R. Simonetta, Joshua Taygerly, Kathleen Boyle, Stephen E. Basham, Chris Padovani, Yan Lou, Thomas J. Cummins, Stephanie L. Yung, Szerenke Kiss von Soly, Frank Kayser, John Kuriyan, Michael Rape, Mario Cardozo, Mark A. Gallop, Neil F. Bence, Paul A. Barsanti, Anjanabha Saha
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Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/1987a6eabdf140cbaf14746bd1ee3135
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spelling oai:doaj.org-article:1987a6eabdf140cbaf14746bd1ee31352021-12-02T15:35:56ZProspective discovery of small molecule enhancers of an E3 ligase-substrate interaction10.1038/s41467-019-09358-92041-1723https://doaj.org/article/1987a6eabdf140cbaf14746bd1ee31352019-03-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-09358-9https://doaj.org/toc/2041-1723Directed protein degradation to target hard-to-drug proteins is a promising therapeutic approach. Here, the authors report the prospective discovery of small molecule “molecular glue” that inserts into a naturally occurring E3 ligase-substrate interface leading to degradation of substrate protein.Kyle R. SimonettaJoshua TaygerlyKathleen BoyleStephen E. BashamChris PadovaniYan LouThomas J. CumminsStephanie L. YungSzerenke Kiss von SolyFrank KayserJohn KuriyanMichael RapeMario CardozoMark A. GallopNeil F. BencePaul A. BarsantiAnjanabha SahaNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Kyle R. Simonetta
Joshua Taygerly
Kathleen Boyle
Stephen E. Basham
Chris Padovani
Yan Lou
Thomas J. Cummins
Stephanie L. Yung
Szerenke Kiss von Soly
Frank Kayser
John Kuriyan
Michael Rape
Mario Cardozo
Mark A. Gallop
Neil F. Bence
Paul A. Barsanti
Anjanabha Saha
Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
description Directed protein degradation to target hard-to-drug proteins is a promising therapeutic approach. Here, the authors report the prospective discovery of small molecule “molecular glue” that inserts into a naturally occurring E3 ligase-substrate interface leading to degradation of substrate protein.
format article
author Kyle R. Simonetta
Joshua Taygerly
Kathleen Boyle
Stephen E. Basham
Chris Padovani
Yan Lou
Thomas J. Cummins
Stephanie L. Yung
Szerenke Kiss von Soly
Frank Kayser
John Kuriyan
Michael Rape
Mario Cardozo
Mark A. Gallop
Neil F. Bence
Paul A. Barsanti
Anjanabha Saha
author_facet Kyle R. Simonetta
Joshua Taygerly
Kathleen Boyle
Stephen E. Basham
Chris Padovani
Yan Lou
Thomas J. Cummins
Stephanie L. Yung
Szerenke Kiss von Soly
Frank Kayser
John Kuriyan
Michael Rape
Mario Cardozo
Mark A. Gallop
Neil F. Bence
Paul A. Barsanti
Anjanabha Saha
author_sort Kyle R. Simonetta
title Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
title_short Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
title_full Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
title_fullStr Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
title_full_unstemmed Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
title_sort prospective discovery of small molecule enhancers of an e3 ligase-substrate interaction
publisher Nature Portfolio
publishDate 2019
url https://doaj.org/article/1987a6eabdf140cbaf14746bd1ee3135
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