Inhibitors of Protein–Protein Interactions
Chapter 2: Target-based Screening and Structure-based Design Approaches to Develop Modulators of Protein–Protein Interactions
Published:25 Nov 2020
Special Collection: 2020 ebook collectionSeries: Chemical Biology
Ashley E. Modell, Paramjit S. Arora, 2020. "Target-based Screening and Structure-based Design Approaches to Develop Modulators of Protein–Protein Interactions", Inhibitors of Protein–Protein Interactions, Ali Tavassoli
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Several complementary approaches have been developed to discover modulators of protein–protein interactions (PPIs). This chapter provides a perspective on bioinformatic classifications of PPIs, which has led to a better understanding of which PPIs are more amenable to modulation. Next, workflows to target PPIs are outlined, including phenotypic screening and target-based approaches. Target-based approaches can be further categorized into structure-based design and target-based screening. The overview, benefits, and drawbacks of each workflow are discussed. Last, we illustrate two complementary computational methods to assess protein interfaces using the KIX protein.