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Protein-Protein Interactions: Are They Now Druggable Targets?
Decision Resources, Inc., Feb 2006, Pages: 20
Protein-protein interactions are central to many key biological pathways and thus are attractive targets for drug discovery. Unfortunately, most efforts thus far to discover small molecules that modulate protein-protein interactions have been unsuccessful, and protein-protein interactions have become known as 'hard targets' and have been dismissed as 'undruggable.' The key question in this field is whether any practical approaches for addressing protein-protein interaction targets can be developed.
This report discusses why protein-protein interactions are so hard to target, describe general strategies for targeting them, and present case studies of protein-protein interaction drug discovery. It also describe projects of three major companies involved in this area and discuss the outlook for this field.
Business Implications
Protein-protein interactions are key to intracellular signaling pathways and cell-surface receptor-ligand interactions. Protein-protein interactions are therefore attractive targets for drug discovery for a host of disease pathways. However, researchers have long considered them to be undruggable 'hard targets.' Except for a few natural products, no marketed drugs target protein-protein interactions.
Researchers have been developing a body of science and technology to enable them to exploit protein-protein interactions as drug targets. The toolkit of technologies aimed at addressing the major challenges in drug discovery for protein-protein interactions encompasses structure-based drug design, peptide-based technologies, combinatorial and medicinal chemistry, fragment-based screening, and whole-pathway cellular assays.
Recently, corporate and academic researchers have discovered several compounds that modulate protein-protein interactions. Companies that have been active in this area include Abbott Laboratories, Ariad Pharmaceuticals, Genentech, GlaxoSmithKline (GSK), Ligand Pharmaceuticals, and Sunesis. The most advanced compounds in this field are thrombopoietin mimetics that arose from a collaboration between Ligand and GSK: eltrombopag (SB-497115) and SB-559448 are in Phase II and Phase I clinical trials, respectively. Preclinical compounds targeting protein-protein interactions in development focus mainly on cancer.
Although research to discover small-molecule drugs that target protein-protein interactions is still at an early stage, we expect to see accelerated activity in this area as compounds move through clinical trials and as the science and technology base continues to develop. The prospect of developing drugs that target biomolecules that are relatively well validated in terms of biological function and role in disease is important in driving advances in this field.
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