Inhibitors of Protein–Protein Interactions
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.
Inhibitors of Protein–Protein Interactions, The Royal Society of Chemistry, 2020.
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Table of contents
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Chapter 1: Identification of Cellular Protein–Protein Interactionsp1-39ByElias Tjärnhage;Elias TjärnhageCurrent address: Institute of Clinical Medicine, University of OsloN-0027 OsloNorwaySearch for other works by this author on:Ylva IvarssonYlva IvarssonSearch for other works by this author on:
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Chapter 2: Target-based Screening and Structure-based Design Approaches to Develop Modulators of Protein–Protein Interactionsp40-65ByAshley E. Modell;Ashley E. ModellDepartment of Chemistry, New York University100 Washington Square EastNew York10003 USA[email protected]Search for other works by this author on:Paramjit S. AroraParamjit S. AroraDepartment of Chemistry, New York University100 Washington Square EastNew York10003 USA[email protected]Search for other works by this author on:
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Chapter 3: The Challenge of Prosecuting Intracellular Protein–Protein Interactions: A Multi-modality Examination of Chemical Matter Identification, Biophysical Characterization, and Membrane Permeabilityp66-110ByL. Fan;L. FanMerck & Co. Inc., Chemistry Capabilities for Accelerating TherapeuticsKenilworth, NJ, 07033USASearch for other works by this author on:W. T. McElroy;W. T. McElroyMerck & Co. Inc., Chemical BiologyKenilworth, NJ07033USASearch for other works by this author on:T. K. Sawyer;T. K. SawyerMerck & Co. Inc., Chemistry Capabilities for Accelerating TherapeuticsBoston, MA02215USASearch for other works by this author on:P. R. Sheth;P. R. ShethMerck & Co. Inc., Screening Target Compound ProfilingKenilworth, NJ07033USASearch for other works by this author on:D. M. TellersD. M. TellersSearch for other works by this author on:
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Chapter 4: Identifying and Developing Small Molecule Inhibitors of Protein–Protein Interactionsp111-159BySamuel E. Dalton;Samuel E. DaltonMerck Sharp & Dohme1st Floor, 2 Pancras SquareLondonNC1 4AGUKSearch for other works by this author on:David C. ReesDavid C. ReesSearch for other works by this author on:
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Chapter 5: Macrocycles as Inhibitors of Protein–Protein Interactionsp160-217ByPierre-Luc Boudreault;Pierre-Luc BoudreaultLaboratoire de Chimie Médicinale, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke3001, 12e av nordSherbrooke (Qc)Canada J1H 5N4[email protected]Search for other works by this author on:Christian Comeau;Christian ComeauLaboratoire de Chimie Médicinale, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke3001, 12e av nordSherbrooke (Qc)Canada J1H 5N4[email protected]Search for other works by this author on:Eric MarsaultEric MarsaultLaboratoire de Chimie Médicinale, Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke3001, 12e av nordSherbrooke (Qc)Canada J1H 5N4[email protected]Search for other works by this author on:
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Chapter 6: Genetically Encoded SICLOPPS Libraries for the Identification of PPI Inhibitorsp218-231ByAli TavassoliAli TavassoliSearch for other works by this author on:
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Chapter 7: RaPID Discovery of Macrocyclic Peptide Inhibitors of Protein–Protein Interactionsp232-246ByR. H. P. van Neer;R. H. P. van NeerDepartment of Chemistry, Graduate School of Science, The University of TokyoBunkyo-kuTokyo113-0033Japan[email protected]Search for other works by this author on:A. A. Vinogradov;A. A. VinogradovDepartment of Chemistry, Graduate School of Science, The University of TokyoBunkyo-kuTokyo113-0033Japan[email protected]Search for other works by this author on:H. SugaH. SugaDepartment of Chemistry, Graduate School of Science, The University of TokyoBunkyo-kuTokyo113-0033Japan[email protected]Search for other works by this author on:
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Chapter 8: Bicyclic Peptide Inhibitors of Protein–Protein Interactionsp247-279ByMarina Buyanova;Marina BuyanovaDepartment of Chemistry and Biochemistry, The Ohio State University484 West 12th AvenueColumbusOhio 43210USA[email protected]Search for other works by this author on:Dehua PeiDehua PeiDepartment of Chemistry and Biochemistry, The Ohio State University484 West 12th AvenueColumbusOhio 43210USA[email protected]Search for other works by this author on:
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Chapter 9: Stapled Peptide Inhibitors of Protein–Protein Interactionsp280-304ByMathias Wendt;Mathias WendtDepartment of Chemistry and Pharmaceutical Sciences, and Amsterdam Institute of Molecular and Life Sciences, VU University AmsterdamDe Boelelaan 11081081 HZ AmsterdamThe Netherlands[email protected]Search for other works by this author on:Niall M. McLoughlin;Niall M. McLoughlinDepartment of Chemistry and Pharmaceutical Sciences, and Amsterdam Institute of Molecular and Life Sciences, VU University AmsterdamDe Boelelaan 11081081 HZ AmsterdamThe Netherlands[email protected]Search for other works by this author on:Tom N. GrossmannTom N. GrossmannDepartment of Chemistry and Pharmaceutical Sciences, and Amsterdam Institute of Molecular and Life Sciences, VU University AmsterdamDe Boelelaan 11081081 HZ AmsterdamThe Netherlands[email protected]Search for other works by this author on:
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Chapter 10: α-Helix Mimetics as Inhibitors of Protein–Protein Interactionsp305-335ByA. J. WilsonA. J. WilsonAstbury Centre for Structural Molecular Biology, University of LeedsWoodhouse LaneLeeds LS2 9JTUKSearch for other works by this author on:
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