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

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

Journal Name: Current Medicinal Chemistry

Volume 28 , Issue 7 , 2021


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Abstract:

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.

Keywords: PROTAC, Small molecule degrader, targeted protein degradation, anticancer therapy, molecular design, diseases.

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Article Details

VOLUME: 28
ISSUE: 7
Year: 2021
Published on: 16 April, 2021
Page: [1304 - 1327]
Pages: 24
DOI: 10.2174/0929867327666200312112412
Price: $65

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