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PROTACs in Treatment of Cancer: A Review

Poonam Arora1, Manjinder Singh1, Varinder Singh1

  • 1Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, Punjab, India.

Mini Reviews in Medicinal Chemistry
|February 26, 2021
PubMed

Insights

PROteolysis targeting chimeras (PROTACs) offer a novel approach to cancer treatment by degrading disease-causing proteins. This review highlights recent PROTAC developments for cancer therapy, addressing drug resistance and relapse challenges.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Cancer treatment faces challenges due to drug resistance and relapse.
  • PROteolysis targeting chimeras (PROTACs) degrade target proteins via the ubiquitin-proteasomal system, offering an alternative to inhibition by small molecules.
  • Despite high potency, no cancer-targeting PROTACs have reached clinical trials.

Purpose of the Study:

  • To review the design, activity, and effects of recently developed PROTACs in cancer.
  • To highlight the potential of PROTAC technology in overcoming cancer treatment resistance.
  • To emphasize the need for further development of PROTACs for viable cancer therapy.

Main Methods:

  • Review of recent scientific literature on PROTAC technology in cancer research.
  • Analysis of PROTAC design strategies and their impact on protein degradation.
  • Evaluation of reported PROTAC activity and efficacy in preclinical cancer models.

Main Results:

  • Several PROTACs demonstrate high potency and activity against cancer targets.
  • PROTACs show promise in degrading disease-causing proteins, potentially overcoming resistance mechanisms.
  • The review covers various PROTAC designs and their observed effects in cancer contexts.

Conclusions:

  • PROTAC technology presents a promising avenue for novel cancer therapeutics.
  • Further research and development are crucial to advance PROTACs into clinical applications for cancer treatment.
  • PROTACs hold significant potential to address unmet needs in oncology, particularly in overcoming drug resistance.
Keywords:
PROTACsanticancercancerproteinstarget.ubiquitin

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