Physical interactions among proteins constitute the backbone of cellular function, making them an attractive source of therapeutic
targets. Although the challenges associated with targeting protein-protein interactions (PPIs) -in particular with small molecules -
are considerable, a growing number of functional PPI modulators is being reported and clinically evaluated. An essential starting point
for PPI inhibitor screening or design projects is the generation of a detailed map of the human interactome and the interactions between
human and pathogen proteins. Different routes to produce these biological networks are being combined, including literature curation and
computational methods. Experimental approaches to map PPIs mainly rely on the yeast two-hybrid (Y2H) technology, which have recently
shown to produce reliable protein networks. However, other genetic and biochemical methods will be essential to increase both
coverage and resolution of current protein networks in order to increase their utility towards the identification of novel disease-related
proteins and PPIs, and their potential use as therapeutic targets.
Keywords: Protein-protein interaction, interactome, drug discovery, small molecule, oncology, virology, PPI modulators, PPI inhibitor, pathogen proteins, yeast two-hybrid (Y2H) technology.
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