Related Experiment Video
Updated: May 10, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
Protein-protein interactions as druggable targets: recent technological advances
Alicia P Higueruelo1, Harry Jubb, Tom L Blundell
1Department of Biochemistry, University of Cambridge, Cambridge CB1 2GA, UK.
Discovering drugs targeting protein-protein interactions (PPI) is challenging. This review explores novel strategies like fragment-based methods and stapled peptides to overcome these hurdles in drug discovery.
Area of Science:
- Drug discovery and medicinal chemistry
- Molecular biology and biochemistry
Background:
- Classical drug discovery methods struggle with protein-protein interactions (PPI).
- Despite challenges, PPI are increasingly recognized as viable drug targets.
- The field of PPI drug discovery is rapidly advancing.
Purpose of the Study:
- To review emerging strategies for targeting protein-protein interactions (PPI).
- To highlight innovative approaches in PPI drug discovery.
Main Methods:
- Fragment-based drug discovery to explore chemical space.
- Stapled peptides for modulating intracellular PPI.
- Alternative inhibition strategies beyond competitive assays.
- Antibody-mediated approaches to facilitate small molecule discovery for PPI.
Main Results:
- New methods demonstrate feasibility of targeting PPI.
- Fragment-based approaches effectively probe PPI chemical space.
- Stapled peptides offer a way to regulate intracellular PPI.
- Antibodies can aid small molecule development for PPI targets.
Conclusions:
- Novel approaches are crucial for successful PPI drug discovery.
- The development of new strategies is accelerating progress in targeting PPI.
- PPI represent a promising frontier for future therapeutics.
More Related Videos
Related Concept Videos
Protein-protein Interfaces
Protein-Protein Interfaces
Protein Networks
These interactions can be represented through maps depicting protein-protein interaction networks, represented as nodes and edges. Nodes are circles that are representative of a protein,...
Protein-Drug Binding: Mechanism and Kinetics
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...
Protein-Drug Binding: Determination Methods
Indirect methods involve isolating the bound drug from its free form in biological samples such as blood, serum, or plasma. These techniques aim to measure the percentage of drugs bound to proteins. Equilibrium dialysis is a commonly used method where the free drug concentration at equilibrium is measured by separating the bound...
Pharmacogenomics: Identification of New Drug Targets

