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Issue 30, 2019
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Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery

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Abstract

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.

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

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Article information


Submitted
07 May 2019
Accepted
14 May 2019
First published
30 May 2019

This article is Open Access

RSC Adv., 2019,9, 16967-16976
Article type
Review Article

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

H. Pei, Y. Peng, Q. Zhao and Y. Chen, RSC Adv., 2019, 9, 16967
DOI: 10.1039/C9RA03423D

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