Main description:

Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.

Contents:

Identification of Cellular Protein-protein Interactions; Target-based Screening and Structure-based Design Approaches to Develop Modulators of Protein-protein Interactions; The Challenge of Prosecuting Intracellular Protein-Protein Interactions: A Multi-Modality Examination of Chemical Matter Identification, Biophysical Characterization, and Membrane Permeability; Identifying and Developing Small Molecule Inhibitors of Protein-protein Interactions; Macrocycles as Inhibitors of Protein-Protein Interactions; Genetically-encoded SICLOPPS Libraries for the Identification of PPI Inhibitors; RaPID Discovery of Macrocyclic Peptide Inhibitors of Protein-protein Interactions; Bicyclic Peptide Inhibitors of Protein-Protein Interactions; Stapled Peptide Inhibitors of Protein-Protein Interactions; -Helix Mimetics as Inhibitors of Protein-Protein Interactions