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Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery

Curing malignant carcinomas is a grand ambition in the development of human health. Over the past decades, targeted therapies have become one of the most successful ways of achieving this. Of these approaches, small molecule inhibitors and monoclonal antibodies are two major methods, however several...

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Detalles Bibliográficos
Autores principales: Pei, Haixiang, Peng, Yangrui, Zhao, Qiuhua, Chen, Yihua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9064693/
https://www.ncbi.nlm.nih.gov/pubmed/35519875
http://dx.doi.org/10.1039/c9ra03423d
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author Pei, Haixiang
Peng, Yangrui
Zhao, Qiuhua
Chen, Yihua
author_facet Pei, Haixiang
Peng, Yangrui
Zhao, Qiuhua
Chen, Yihua
author_sort Pei, Haixiang
collection PubMed
description Curing malignant carcinomas is a grand ambition in the development of human health. Over the past decades, targeted therapies have become one of the most successful ways of achieving this. Of these approaches, small molecule inhibitors and monoclonal antibodies are two major methods, however several barriers to their development and clinical use still exist. The use of proteolysis-targeting chimeras (PROTACs) is a new technology through utilizing a intracellular ubiquitin-proteasome system to induce targeted protein degradation, is receiving much attention in the field of targeted therapies. Hetero-bifunctional PROTACs have the potential to eliminate the “undruggable” proteome that comprises about 85% of human proteins, which indicates their great prospects in therapeutic fields. However, there are some hurdles preventing current PROTACs moving from bench to clinic, such as delivery and bioavailability. This review provides an overview of the development of PROTAC technology and will briefly summarize the future possible directions of this approach.
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spelling pubmed-90646932022-05-04 Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery Pei, Haixiang Peng, Yangrui Zhao, Qiuhua Chen, Yihua RSC Adv Chemistry Curing malignant carcinomas is a grand ambition in the development of human health. Over the past decades, targeted therapies have become one of the most successful ways of achieving this. Of these approaches, small molecule inhibitors and monoclonal antibodies are two major methods, however several barriers to their development and clinical use still exist. The use of proteolysis-targeting chimeras (PROTACs) is a new technology through utilizing a intracellular ubiquitin-proteasome system to induce targeted protein degradation, is receiving much attention in the field of targeted therapies. Hetero-bifunctional PROTACs have the potential to eliminate the “undruggable” proteome that comprises about 85% of human proteins, which indicates their great prospects in therapeutic fields. However, there are some hurdles preventing current PROTACs moving from bench to clinic, such as delivery and bioavailability. This review provides an overview of the development of PROTAC technology and will briefly summarize the future possible directions of this approach. The Royal Society of Chemistry 2019-05-30 /pmc/articles/PMC9064693/ /pubmed/35519875 http://dx.doi.org/10.1039/c9ra03423d Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
Pei, Haixiang
Peng, Yangrui
Zhao, Qiuhua
Chen, Yihua
Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title_full Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title_fullStr Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title_full_unstemmed Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title_short Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
title_sort small molecule protacs: an emerging technology for targeted therapy in drug discovery
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9064693/
https://www.ncbi.nlm.nih.gov/pubmed/35519875
http://dx.doi.org/10.1039/c9ra03423d
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