Modulating Protein-Protein Interactions for Drug Discovery

Dear Colleagues,

Proteins regulate many fundamental processes in living cells, including transcription, splicing, translation, protein folding/degradation, cytokinesis and signaling. They rarely fulfill their functions alone, but rather associate with other proteins in cells. Aberrant protein-protein interactions (PPIs) lead to human diseases. Small molecules or peptidomimetics to reverse the aberrant role of PPIs can be developed into therapeutics. The disruption of PPIs with small molecules is considered difficult due to the large and flat interaction surface, which lacks a druggable binding pocket. A wide range of methods and technologies have been developed to tackle this challenge, including small-molecule library synthesis and construction, biophysical/biochemical/cellular assay development and screening technologies, as well as computational approaches. Tremendous efforts in the past two decades have led to the approval of a few drugs that disrupt PPIs in the clinic. In addition to disrupting PPIs, small molecules have been found to enable neo-PPIs to degrade traditionally considered undruggable proteins, either by rational design or serendipity, such as proteolysis-targeting chimeras (PROTACs), molecular glues and other protein degradation modalities. PPI modulation is still in its early stage, and provides opportunities for developing therapeutics to treat human diseases.

Researchers in the field of drug discovery and chemical biology are invited to contribute review and original research articles to this Special Issue related to protein-protein interactions, using both computational and experimental methods.

Dr. Hao Shao
Guest Editor

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