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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Nature Portfolio
2019
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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) |
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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 |
work_keys_str_mv |
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