Advancing Strategies for Proteolysis-Targeting Chimera Design

  • J Med Chem. 2023 Feb 23;66(4):2308-2329. doi: 10.1021/acs.jmedchem.2c01555.
Minglei Li  1 Ying Zhi  1 Bo Liu  1 Qingqiang Yao  1
Affiliations
  • 1. School of Pharmacy and Pharmaceutical Sciences, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, 250117 Shandong, P. R. China.
Abstract

Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by degrading various disease-causing proteins, particularly those related to tumors. Therefore, the introduction of PROTACs has ushered in a new chapter of antitumor drug development, marked by significant advances over recent years. Herein, we describe recent developments in PROTAC technology, focusing on design strategy, development workflow, and future outlooks. We also discuss potential opportunities and challenges for PROTAC research.

Products