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Targeting conventionally intractable cancer-driving proteins: What has been achieved recently?

Qifeng Xie1, Wenqiang Xu1, Yang Wang2

  • 1Department of Medicinal Chemistry, School of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, China.

European Journal of Medicinal Chemistry
|June 27, 2026
PubMed

Insights

Developing new drugs for "undruggable" cancer targets like transcription factors and GTPases is advancing rapidly. Recent breakthroughs offer hope for novel cancer therapies against these challenging oncoproteins.

Area of Science:

  • Oncology
  • Drug Discovery
  • Molecular Biology

Background:

  • Many cancer-driving proteins are difficult to target with traditional drugs.
  • Challenges include protein structure and function, making them

Purpose of the Study:

  • To review strategies for targeting four classes of undruggable oncoproteins.
  • To highlight key targets within each class.
  • To provide perspectives for future drug discovery.

Main Methods:

  • Literature review of drug design strategies and experimental techniques.
  • Analysis of progress in targeting transcription factors, GTPases, scaffolding proteins, and phosphatases.
  • Focus on successful examples and emerging approaches.

Main Results:

  • Significant progress has been made in developing therapeutics for previously intractable oncoproteins.
  • Approved KRASG12C inhibitors represent a major achievement.
  • Investigational drugs and potent in vivo therapeutics are emerging.

Conclusions:

  • Innovative strategies are overcoming challenges in targeting undruggable oncoproteins.
  • This field is rapidly advancing, offering new hope for cancer treatment.
  • The overview aims to guide future research and drug development.
Keywords:
CancerDrug designStrategic stridesUndruggable

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