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

(E-pub Ahead of Print)

Author(s): Zere Mukhamejanova, Yichen Tong, Qi Xiang, Fang Xu, Jiyan Pang*.

Journal Name: Current Medicinal Chemistry


(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.

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

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(E-pub Ahead of Print)
DOI: 10.2174/0929867327666200312112412
Price: $95

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