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The Future of Medicinal Chemistry, PROTAC, and Undruggable Drug Targets

Antti Poso1,2

  • 1School of Pharmacy, University of Eastern Finland, P.O. BOX 1627, 70211 Kuopio, Finland.

Journal of Medicinal Chemistry
|July 23, 2021
PubMed

Insights

New Proteolysis Targeting Chimeras (PROTACs) enable the inactivation of WRD5, a key target in epigenetic regulation and anticancer drug discovery. This facilitates the evaluation of WRD5 as a viable therapeutic target.

Area of Science:

  • Oncology
  • Epigenetics
  • Medicinal Chemistry

Background:

  • WRD5 is implicated in epigenetic regulation.
  • WRD5 presents a promising target for anticancer drug discovery.
  • Classical methods for WRD5 inactivation are challenging.

Purpose of the Study:

  • To introduce novel WRD5-targeting Proteolysis Targeting Chimeras (PROTACs).
  • To assess the therapeutic potential of WRD5 as a drug target.

Main Methods:

  • Development of novel PROTACs designed to target WRD5.
  • In vitro and cellular activity assessments of the developed PROTACs.

Main Results:

  • Successfully synthesized novel WRD5-targeting PROTACs.
  • Demonstrated cellular activity of the new PROTAC compounds.

Conclusions:

  • The developed PROTACs provide a viable tool for WRD5 inactivation.
  • These findings support the evaluation of WRD5 as a drug target in cancer therapy.

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