Cargando…
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...
Autores principales: | , , , |
---|---|
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 |
_version_ | 1784699437618036736 |
---|---|
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. |
format | Online Article Text |
id | pubmed-9064693 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT peihaixiang smallmoleculeprotacsanemergingtechnologyfortargetedtherapyindrugdiscovery AT pengyangrui smallmoleculeprotacsanemergingtechnologyfortargetedtherapyindrugdiscovery AT zhaoqiuhua smallmoleculeprotacsanemergingtechnologyfortargetedtherapyindrugdiscovery AT chenyihua smallmoleculeprotacsanemergingtechnologyfortargetedtherapyindrugdiscovery |