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

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 KRAS^G12C 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.