2. Academic Validation
  3. Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation

Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation

  • Eur J Med Chem. 2019 Jul 15:174:159-180. doi: 10.1016/j.ejmech.2019.04.036.
Meiyang Xi 1,  Yi Chen 1,  Hongyu Yang 2,  Huiting Xu 1,  Kui Du 1,  Chunlei Wu 1,  Yanfei Xu 1,  Liping Deng 1,  Xiang Luo 1,  Lemao Yu 1,  Yonghua Wu 1,  Xiaozhong Gao 1,  Tao Cai 1,  Bin Chen 1,  Runpu Shen 3,  Haopeng Sun 4
Affiliations

Affiliations

  • 1 College of Chemistry and Chemical Engineering, Shaoxing University, Shaoxing, 312000, China.
  • 2 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
  • 3 College of Chemistry and Chemical Engineering, Shaoxing University, Shaoxing, 312000, China. Electronic address: srunpu@usx.edu.cn.
  • 4 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: sunhaopeng@163.com.
PMID: 31035238 DOI: 10.1016/j.ejmech.2019.04.036
Abstract

Inhibitors and nucleic acid based techniques were two main approaches to interfere with protein signaling and respective cascade in the past. Until recently, a new class of small molecules named proteolysis-targeting chimeras (PROTACs) have emerged. Each contains a target warhead, a linker and an E3 ligand. These bifunctional molecules recruit E3 Ligases and target specific proteins for degradation via the ubiquitin (Ub) Proteasome system (UPS). The degradation provides several advantages over inhibition in potency, selectivity and drug resistance. Thus, a variety of small molecule PROTACs have been discovered so far. In this review, we summarize the biological mechanism, advantages and recent progress of PROTACs, trying to offer an outlook in development of drugs targeting degradation in future.

Keywords

Degradation; E3 ligase; PROTACs; Proteasome.

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