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The PROTAC technology in drug development.

Yutian Zou1,2, Danhui Ma1, Yinyin Wang1

  • 1The State Laboratory of Membrane Biology, Department of Basic Medicine, School of Medicine, Tsinghua University, Beijing, China.

Cell Biochemistry and Function
|January 4, 2019
PubMed
Summary

Proteolysis targeting chimera (PROTAC) technology induces targeted protein degradation. This review highlights PROTAC

Keywords:
PROTACcancerdrug developmentprotein degradationsmall molecule

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Proteolysis targeting chimera (PROTAC) is an emerging technology for targeted protein degradation.
  • PROTACs utilize a hybrid molecule to recruit E3 ubiquitin ligase to a target protein, leading to its ubiquition and subsequent degradation.
  • The development of PROTAC technology has been driven by several key research groups over the past decade.

Purpose of the Study:

  • To review the historical development and contributions of key groups in PROTAC technology.
  • To provide an overview of PROTAC applications in various diseases, with a focus on cancer therapy.
  • To offer expert opinions on the future potential of PROTACs in oncology.

Main Methods:

  • Literature review of PROTAC development and applications.
  • Analysis of contributions from pioneering research groups.
  • Synthesis of current research trends and future perspectives in PROTAC technology.

Main Results:

  • The review details the foundational work and evolution of PROTAC technology.
  • It highlights the expansion of PROTAC applications beyond initial targets to diverse diseases, including various cancers.
  • The study underscores the collaborative efforts that have advanced this innovative therapeutic modality.

Conclusions:

  • PROTAC technology represents a significant advancement in targeted protein degradation strategies.
  • Its application in cancer therapy holds considerable promise for developing novel anti-cancer drugs.
  • Continued research and development are expected to further expand the therapeutic utility of PROTACs.