Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development

PROTACs employ the proteosome-mediated proteolysis via E3 ligase and recruit the natural protein degradation machinery to selectively degrade the cancerous proteins. Herein, we have designed and synthesized heterobifunctional small molecules that consist of different linkers tethering KRIBB11, a HSF...

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Detalles Bibliográficos
Autores principales: Sharma, Chiranjeev, Choi, Myeong A, Song, Yoojin, Seo, Young Ho
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8912087/
https://www.ncbi.nlm.nih.gov/pubmed/35268755
http://dx.doi.org/10.3390/molecules27051655
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author Sharma, Chiranjeev
Choi, Myeong A
Song, Yoojin
Seo, Young Ho
author_facet Sharma, Chiranjeev
Choi, Myeong A
Song, Yoojin
Seo, Young Ho
author_sort Sharma, Chiranjeev
collection PubMed
description PROTACs employ the proteosome-mediated proteolysis via E3 ligase and recruit the natural protein degradation machinery to selectively degrade the cancerous proteins. Herein, we have designed and synthesized heterobifunctional small molecules that consist of different linkers tethering KRIBB11, a HSF1 inhibitor, with pomalidomide, a commonly used E3 ligase ligand for anticancer drug development.
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spelling pubmed-89120872022-03-11 Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development Sharma, Chiranjeev Choi, Myeong A Song, Yoojin Seo, Young Ho Molecules Article PROTACs employ the proteosome-mediated proteolysis via E3 ligase and recruit the natural protein degradation machinery to selectively degrade the cancerous proteins. Herein, we have designed and synthesized heterobifunctional small molecules that consist of different linkers tethering KRIBB11, a HSF1 inhibitor, with pomalidomide, a commonly used E3 ligase ligand for anticancer drug development. MDPI 2022-03-02 /pmc/articles/PMC8912087/ /pubmed/35268755 http://dx.doi.org/10.3390/molecules27051655 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sharma, Chiranjeev
Choi, Myeong A
Song, Yoojin
Seo, Young Ho
Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title_full Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title_fullStr Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title_full_unstemmed Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title_short Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development
title_sort rational design and synthesis of hsf1-protacs for anticancer drug development
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8912087/
https://www.ncbi.nlm.nih.gov/pubmed/35268755
http://dx.doi.org/10.3390/molecules27051655
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