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Updated: Dec 24, 2025

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
Small-molecule PROTACs: novel agents for cancer therapy
Yichao Wan1, Chunxing Yan1, Han Gao1
1Key Laboratory of Theoretical Organic Chemistry & Functional Molecule, Ministry of Education, Hunan Provincial Key Laboratory of Controllable Preparation & Functional Application of Fine Polymers, School of Chemistry & Chemical Engineering, Hunan University of Science & Technology, Xiangtan, Hunan, 411201, PR China.
Abstract:
Proteolysis-targeting chimera (PROTAC) is a new technology to selectively degrade target proteins via ubiquitin-proteasome system. PROTAC molecules (PROTACs) are a class of heterobifunctional molecules, which contain a ligand targeting the protein of interest, a ligand recruiting an E3 ligase and a linker connecting these two ligands. They provide several advantages over traditional inhibitors in potency, selectivity and drug resistance. Thus, many promising PROTACs have been developed in the recent two decades, especially small-molecule PROTACs. In this review, we briefly introduce the mechanism of PROTACs and focus on the progress of small-molecule PROTACs based on different E3 ligases. In addition, we also introduce the opportunities and challenges of small-molecule PROTACs for cancer therapy.
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