Review

Nature Reviews Drug Discovery 3, 301-317 (April 2004) | doi:10.1038/nrd1343

Small-molecule inhibitors of protein–protein interactions: progressing towards the dream

Michelle R. Arkin1 & James A. Wells1  About the authors

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Protein–protein interactions have a key role in most biological processes, and offer attractive opportunities for therapeutic intervention. Developing small molecules that modulate protein–protein interactions is difficult, owing to issues such as the lack of well-defined binding pockets. Nevertheless, there has been important progress in this endeavour in recent years. Here, we use illustrative examples to discuss general strategies for addressing the challenges inherent in the discovery and characterization of small-molecule inhibitors of protein–protein interactions.

Author affiliations

  1. Sunesis Pharmaceuticals, 341 Oyster Point Boulevard, South San Francisco, California 94080, USA.
    Email: mra@sunesis.com
    Email: jaw@sunesis.com

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