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Targeted Cancer Therapies02:57

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Related Experiment Video

Updated: Apr 6, 2026

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
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Contemporary Developments in PROTACs for Cancer Management: An In-Depth Review.

Shaik Abdul Rahaman1, Garla Venkateswarlu2, Sakshi Patel1,3

  • 1School of Medical and Allied Sciences, Department of Pharmacy, Galgotias University, Uttar Pradesh, 203201, India.

Current Topics in Medicinal Chemistry
|April 5, 2026
PubMed
Summary

Proteolysis-Targeting Chimeras (PROTACs) offer a new way to treat cancer by degrading disease-causing proteins. Recent advancements show PROTACs are effective in early trials, with ongoing work to overcome challenges and improve their therapeutic potential.

Keywords:
Cancer managementDrug discovery.E3 LigasesOncologyPROTAC (proteolysis-targeting chimeras)Targeted protein degradation

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Proteolysis-Targeting Chimeras (PROTACs) are a novel therapeutic strategy.
  • PROTACs degrade disease-causing proteins using the ubiquitin proteasome system.
  • They offer an alternative to conventional small-molecule inhibitors for various cancers.

Purpose of the Study:

  • To review recent developments in PROTAC technology.
  • To discuss the applications of PROTACs in oncology.
  • To highlight challenges and future directions for PROTACs in cancer therapy.

Main Methods:

  • Review of recent scientific literature on PROTACs.
  • Analysis of PROTAC design, pharmacokinetics, and clinical trial data.
  • Discussion of E3 ligase versatility and delivery innovations.

Main Results:

  • PROTACs show efficacy in preclinical models of solid tumors and hematologic malignancies.
  • Initial clinical trials demonstrate the potential of PROTACs in human patients.
  • Improvements in PROTAC stability, bioavailability, and delivery are enabling clinical translation.

Conclusions:

  • PROTACs are a promising strategy for addressing unmet needs in oncology.
  • Further research is needed to reduce off-target effects and overcome resistance.
  • Optimizing PROTAC design and exploring combination therapies are key future directions.