Design, Discovery and Development of Modulators Targeting Protein-Protein Interactions

Dear Colleagues,

The human proteome comprises approximately 20,000 proteins, and protein–protein interactions (PPIs) play pivotal roles in biological processes. Their dysregulation often results in the onset and progression of several diseases. Therefore, PPIs represent promising drug discovery targets. Historically, PPIs were considered to be “undruggable” with their large and flat binding surfaces being smooth and lacking well-defined binding pockets. Targeting these is a challenging task when attempting to convert drug-like small molecules to therapeutics due to the fact that PPI interfaces exhibit different biochemical and biophysical properties relative to the small molecule compound binding pockets. Natural products, derivatives thereof, peptides, and peptidomimetics represent other sources for the modulation of PPIs. We invite authors to submit original research and review articles regarding the molecular aspects, including, but not limited to, the following topics:

— Some examples of targeted PPIs:

• Bcl-2 family PPIs (cancer)
• p53–MDM2 (cancer)
• RKIP(Raf kinase inhibitory protein)—C-Raf(Raf-1 kinase) (cancer and Alzheimer’s disease)
• Keap1–Nrf2 (cancer)

— The goal of the issue is to highlight:

• Recent advances in understanding and mastering PPIs as drug discovery targets;
• Targeting PPIs with:

1. Small molecules;
2. Peptides and peptidomimetics;

• Natural products and derivatives thereof.

Dr. Konstantinos Agrios
Guest Editor

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