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…mehr
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.
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
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
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