PROTAC: A promising technology for cancer treatment

Eur J Med Chem. 2020 Oct 1:203:112539. doi: 10.1016/j.ejmech.2020.112539.

Xin Zhou ¹, Ru Dong ¹, Jin-Yang Zhang ¹, Xin Zheng ¹, Li-Ping Sun ²

Affiliations

1 Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, PR China.
2 Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, PR China. Electronic address: [email protected].

PMID: 32698111 DOI: 10.1016/j.ejmech.2020.112539

Abstract

Proteolysis-targeting chimeric molecules (PROTACs), which attract much more attention today, may be a potential way to treat Cancer. PROTACs are made up of ligands of target proteins, E3 Ligase recruiting elements and linkers. PROTACs can hijack the intracellular inherent ubiquitin Proteasome system in cells to degrade different target proteins. PROTACs targeting different cancer-related proteins have been successfully developed and outperform small inhibitors, the traditional way of treating Cancer. In this review, we focus on PROTACs targeting cancer-related proteins and their superiority over inhibitors.

Keywords

Cancer; PROTACs; Promising treatment.

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