Zere Mukhamejanova, Yichen Tong , Qi Xiang, Fang Xu* and Jiyan Pang* Pages 1304 - 1327 ( 24 )
PROTAC (Proteolysis Targeting Chimera) degraders based on protein knockdown technology are now suggested as a novel option for the treatment of various diseases. Over the last couple of years, the application of PROTAC technology has spread in a wide range of disorders, and plenty of PROTAC molecules with high potency have been reported. Mostly developing for anticancer therapy, these molecules showed high selectivities to target proteins, the ability to significantly induce degradation of oncoproteins, good in vitro and in vivo results. In this review, we summarized the recent development of PROTAC technology in the anticancer therapy field, including molecular design, types of targeted proteins, in vitro and in vivo results. Additionally, we also discuss the prospects and challenges for the application of candidates based on PROTAC strategy in clinical trials.
PROTAC, Small molecule degrader, targeted protein degradation, anticancer therapy, molecular design, diseases.
School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, Institute of Biomedicine & Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou 510632, School of Chemistry, Sun Yat-Sen University, Guangzhou 510275