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New genomic information has revealed the crucial role that protein-protein interactions (PPIs) play in regulating numerous cellular functions. Aberrant forms of these interactions are common in numerous diseases and thus PPIs have emerged as a vast class of critical drug targets. Despite the importance of PPIs in biology, it has been extremely challenging to convert targets into therapeutics and targeting PPIs had long been considered a very difficult task. However, over the past decade the field has advanced with increasing growth in the number of successful PPI regulators. Protein-Protein Interaction Regulators surveys the latest advances in the structural understanding of PPIs as well as recent developments in modulator discovery.
List of contents
Introduction; Protein-protein interaction interfaces and their functional implications; Protein-Protein interaction networks in human disease; High Throughput Screening Methods for PPI inhibitor discovery; Computational structural modeling to discover PPI modulators; Small molecule inhibitors of E3 ubiquitin ligases; Hydrogen bond surrogate stabilized helices as Protein-Protein interaction inhibitors; Helix-mimetics as Protein-Protein Interaction Inhibitors; Discovery and Development of Mcl-1 Inhibitors as Anti-cancer Therapeutics: Hit to Clinical Candidate Optimization; Pharmacological Regulation and Functional Significance of Chromatin Binding by BET Tandem Bromodomains; Small-molecule modulators of Protein-Protein Interactions: focus on 14-3-3 PPIs; Discovery of AMG 232, a small molecule MDM2 inhibitor in clinical development and its back-up clinical candidate, AM-7209; Small Molecule Inhibitors of Myc-Max Interaction and DNA Binding; Small Molecule Modulators of Endo-Lysosomal Toll-Like Receptors
Summary
Protein–Protein Interaction Regulators surveys the latest advances in the structural understanding of PPIs as well as recent developments in modulator discovery.
