Inhibitors of Protein-Protein Interactions

Dear Colleagues,

 The human body has nearly fifty thousand proteins that interact with one another to perform the functions of the body. The association of two proteins could result in homodimers or heterodimers in the cellular environment. These proteins are responsible for most of the biochemical pathways that control the physiological processes. Deregulation of protein-protein interaction may result in a disease state. Protein–protein interactions (PPI) can be inhibited by antibodies, small molecules, or peptides, and inhibition of PPI has therapeutic value. During the last decade, PPI drug discovery research has steadily increased, and a few PPI inhibitors have already reached the pharmaceutical market. Contributions in structural biology research resulted in  significant progress in the design of PPI inhibitors. As structures of the physiologically important proteins and protein complexes were elucidated by experimental and computational methods, and interactions of proteins were deciphered, it was realized that protein-protein interaction surfaces are important in modulating the physiological processes for alleviating many disease states. What was once assumed as the undruggable target is now gaining interest. The bottleneck in PPI drug discovery is the availability of the three-dimensional structure of PPI complexes, as only a few complex protein structures are available. Advances in molecular biology, computational biology methods, and cryo-electron microscopy have contributed to the methods of deciphering the structure of protein complexes. New methods to study PPI and its inhibition are reported. Although there are challenges in PPI drug design, it is a rapidly-growing area with many pharmaceutical companies participating in PPI drug discovery. In this Special Issue on PPI inhibition, our focus is on the structure of protein complexes that have a druggable interface area, experimental methods to detect PPI and its inhibition, and PPI inhibitors that are on the market or pipeline.   

Prof. Dr. Seetharama D. S. Jois
Guest Editor

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• protein-protein interaction
• assay development
• drug discovery
• structural biology