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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Bibliographic Details
Published in:RSC advances 2019-05, Vol.9 (3), p.16967-16976
Main Authors: Pei, Haixiang, Peng, Yangrui, Zhao, Qiuhua, Chen, Yihua
Format: Article
Language:English
Subjects:
Bioavailability
Chemistry
Monoclonal antibodies
New technology
Proteins
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Summary: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. An overview of the latest developments in PROTAC technology and the possible directions of this approach is presented.
ISSN:2046-2069
2046-2069
DOI:10.1039/c9ra03423d