Abstract
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.
Current Pharmaceutical Design
Title:Protein-protein Interactions: Network Analysis and Applications in Drug Discovery
Volume: 18 Issue: 30
Author(s): Jennyfer Bultinck, Sam Lievens and Jan Tavernier
Affiliation:
Keywords: Protein-protein interaction, interactome, drug discovery, small molecule, oncology, virology, PPI modulators, PPI inhibitor, pathogen proteins, yeast two-hybrid (Y2H) technology.
Abstract: 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.
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Cite this article as:
Bultinck Jennyfer, Lievens Sam and Tavernier Jan, Protein-protein Interactions: Network Analysis and Applications in Drug Discovery, Current Pharmaceutical Design 2012; 18 (30) . https://dx.doi.org/10.2174/138161212802651562
DOI https://dx.doi.org/10.2174/138161212802651562 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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