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Recent Advances in the Design and Development of Anticancer Molecules Based on PROTAC Technology


Zere Mukhamejanova, Yichen Tong , Qi Xiang, Fang Xu and Jiyan Pang*   Pages 1 - 24 ( 24 )


(Proteolysis targeting chimera) degraders based on protein knockdown technology now are suggested as a novel option for the treatment of various diseases. Over the last couple of years, 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 show high selectivity to target proteins, ability to significantly induce degradation of oncoproteins, good in vivo and in vitro 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 vivo and in vitro data results. Additionally, we also discuss on the prospects and challenges for application of candidates based on PROTAC strategy in clinical trials.


PROTAC, small molecule degrader, targeted protein degradation, anticancer therapy


Sun Yat-Sen University, School of Chemistry, Sun Yat-Sen University, School of Chemistry , Jinan University, Institute of Biomedicine & Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, 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, Sun Yat-Sen University, School of Chemistry

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