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Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery
Haixiang Pei1, Yangrui Peng1, Qiuhua Zhao2
1Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences, School of Life Sciences, East China Normal University Shanghai 200241 China yhchen@bio.ecnu.edu.cn.
RSC Advances
|May 6, 2022
Summary
Proteolysis-targeting chimeras (PROTACs) offer a novel approach to targeted cancer therapy by degrading disease-causing proteins. While promising for the "undruggable" proteome, challenges in delivery and bioavailability must be overcome for clinical success.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Targeted therapies, including small molecule inhibitors and monoclonal antibodies, have advanced cancer treatment.
- Existing targeted therapies face limitations in development and clinical application.
- The proteome, comprising approximately 85% of human proteins, remains largely "undruggable" with conventional methods.
Purpose of the Study:
- To provide an overview of proteolysis-targeting chimera (PROTAC) technology development.
- To highlight the potential of PROTACs in targeted protein degradation for therapeutic applications.
- To summarize future directions and challenges for PROTACs in clinical settings.
Main Methods:
- Review of existing literature on PROTAC technology.
- Discussion of the mechanism of action of PROTACs utilizing the ubiquitin-proteasome system.
- Analysis of the potential and limitations of hetero-bifunctional PROTACs.
Main Results:
- PROTACs represent a novel therapeutic strategy for targeted protein degradation.
- Hetero-bifunctional PROTACs show potential in targeting previously "undruggable" proteins.
- Current PROTAC technology faces hurdles such as delivery and bioavailability.
Conclusions:
- PROTACs hold significant promise for advancing targeted cancer therapies.
- Overcoming challenges in delivery and bioavailability is crucial for clinical translation of PROTACs.
- Further research into PROTAC development could unlock new therapeutic avenues for various diseases.
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