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Updated: Apr 15, 2026
Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
[Chemical libraries dedicated to protein-protein interactions]
Olivier Sperandio1, Bruno O Villoutreix1, Xavier Morelli2
1Molécules thérapeutiques in silico (MTi), université Paris Diderot, Inserm UMR-S973, 35, rue Hélène Brion, 75205 Paris Cedex 13, France.
Protein-protein interactions (PPI) are crucial in biology and disease, presenting therapeutic opportunities. This review highlights efforts in developing chemical libraries to target these challenging protein-protein interactions for drug discovery.
Area of Science:
- Molecular Biology
- Biochemistry
- Pharmacology
Context:
- Protein-protein interactions (PPI) are fundamental to cellular processes, including biological pathways, host-pathogen interactions, and cancer.
- PPI represent a significant, yet challenging, class of targets for drug discovery programs.
- Understanding the structural and physicochemical properties of protein-protein interfaces is key to developing effective inhibitors.
Purpose:
- To review current strategies and efforts in developing chemical libraries specifically designed for targeting protein-protein interactions (PPI).
- To provide an overview of the progress made in characterizing PPI and their interfaces for therapeutic intervention.
- To showcase the development of PPI-focused chemical libraries.
Summary:
- Recent advancements have enabled the characterization of protein-protein interfaces, facilitating the design of small molecules to disrupt PPI.
- The development of PPI inhibitors has led to the creation of specialized chemical libraries.
- This review consolidates current research on building chemical libraries tailored for PPI targets.
Impact:
- Enables the development of novel therapeutics by providing targeted chemical libraries for challenging PPI targets.
- Advances drug discovery by offering insights into the structural basis of PPI inhibition.
- Facilitates a deeper understanding of cellular mechanisms and disease pathways involving PPI.
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