PROTAC: A promising technology for cancer treatment

Xin Zhou; Ru Dong; Jin-Yang Zhang; Xin Zheng; Li-Ping Sun

doi:10.1016/j.ejmech.2020.112539

PROTAC: A promising technology for cancer treatment

Eur J Med Chem. 2020 Oct 1:203:112539. doi: 10.1016/j.ejmech.2020.112539. Epub 2020 Jul 15.

Authors

Xin Zhou¹, Ru Dong¹, Jin-Yang Zhang¹, Xin Zheng¹, Li-Ping Sun²

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: chslp@cpu.edu.cn.

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.

Publication types

Review

MeSH terms

Animals
Antineoplastic Agents / pharmacology*
Antineoplastic Agents / therapeutic use
Humans
Intracellular Space / drug effects
Intracellular Space / metabolism
Molecular Targeted Therapy / methods*
Neoplasms / drug therapy*
Neoplasms / metabolism
Neoplasms / pathology
Proteolysis / drug effects*

Substances

Antineoplastic Agents