Protein-protein interaction modulators: advances, successes and remaining challenges

Area of Science:

• Medicinal Chemistry
• Molecular Biology
• Drug Discovery

Background:

• Protein-protein interactions (PPIs) are key targets for disease intervention.
• Targeting intracellular PPIs presents challenges due to their large, dynamic interfaces.
• Small-molecule inhibitors offer a promising strategy for modulating PPIs.

Purpose of the Study:

• To review advances in small-molecule-based modulation of PPIs.
• To highlight successes and challenges in PPI-focused drug discovery.
• To discuss the therapeutic potential of PPI modulators in disease.

Main Methods:

• Literature review of PPI-focused drug discovery.
• Analysis of current small-molecule inhibitors targeting PPIs.
• Examination of clinical trial data for PPI modulators.

Main Results:

• Several small-molecule drugs targeting PPIs are on the market or in clinical trials.
• Advances in drug discovery technologies have improved the targeting of PPIs.
• Significant progress has been made in developing PPI modulators for therapeutic applications.

Conclusions:

• Small molecules are effective modulators of disease-relevant PPIs.
• Despite inherent challenges, PPIs represent a viable target class for drug development.
• Continued research in PPI-focused drug discovery holds promise for future therapeutics.