Protein – Protein Interaction Regulators
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.
Protein – Protein Interaction Regulators, The Royal Society of Chemistry, 2020.
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Table of contents
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CHAPTER 1: Protein–Protein Interaction Interfaces and their Functional Implicationsp1-24ByG. SchreiberG. SchreiberSearch for other works by this author on:
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CHAPTER 2: Protein–Protein Interaction Networks in Human Diseasep25-48ByBrandon S. Dunn;Brandon S. DunnDepartment of Epigenetics and Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center1808 Park Road 1CSmithvilleTXUSA[email protected]Search for other works by this author on:Sharad Awasthi;Sharad AwasthiDepartment of Epigenetics and Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center1808 Park Road 1CSmithvilleTXUSA[email protected]Search for other works by this author on:S. Stephen Yi;S. Stephen YiDepartment of Oncology, Dell Medical School, The University of Texas at AustinAustinTXUSADepartment of Biomedical Engineering, Cockrell School of Engineering, The University of Texas at AustinAustinTXUSASearch for other works by this author on:Nidhi SahniNidhi SahniDepartment of Epigenetics and Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center1808 Park Road 1CSmithvilleTXUSA[email protected]Department of Bioinformatics and Computational Biology, The University of Texas MD Anderson Cancer CenterHoustonTXUSAProgram in Quantitative and Computational Biosciences (QCB), Baylor College of MedicineHoustonTXUSASearch for other works by this author on:
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CHAPTER 3: High Throughput Screening Methods for PPI Inhibitor Discoveryp49-86BySean P. Doyle;Sean P. DoyleMolecular and Systems Pharmacology Graduate Program, Emory UniversityAtlantaGA 30322USA[email protected]Department of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:Xiulei Mo;Xiulei MoDepartment of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USAEmory Chemical Biology Discovery Center, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:Kun Qian;Kun QianDepartment of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USAEmory Chemical Biology Discovery Center, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:Danielle N. Cicka;Danielle N. CickaMolecular and Systems Pharmacology Graduate Program, Emory UniversityAtlantaGA 30322USA[email protected]Department of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:Qiankun Niu;Qiankun NiuDepartment of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USAEmory Chemical Biology Discovery Center, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:Haian FuHaian FuDepartment of Pharmacology and Chemical Biology, Emory University School of MedicineAtlantaGA 30322USAEmory Chemical Biology Discovery Center, Emory University School of MedicineAtlantaGA 30322USASearch for other works by this author on:
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CHAPTER 4: Computational Structural Modeling to Discover PPI Modulatorsp87-108ByXuan Yang;Xuan YangDepartment of Pharmacology and Chemical Biology, Emory University School of Medicine, Emory UniversityAtlantaGAUSA[email protected]Emory Chemical Biology Discovery Center, Emory University School of Medicine, Emory UniversityAtlantaGAUSASearch for other works by this author on:Andrey A. IvanovAndrey A. IvanovDepartment of Pharmacology and Chemical Biology, Emory University School of Medicine, Emory UniversityAtlantaGAUSA[email protected]Emory Chemical Biology Discovery Center, Emory University School of Medicine, Emory UniversityAtlantaGAUSAWinship Cancer Institute, Emory UniversityAtlantaGAUSASearch for other works by this author on:
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CHAPTER 5: Small Molecule Inhibitors of E3 Ubiquitin Ligasesp109-123ByNobumoto Watanabe;Nobumoto WatanabeBioprobe Application Research Unit, RIKEN Center for Sustainable Resource ScienceWakoSaitama351-0198 Japan[email protected]Search for other works by this author on:Hiroyuki OsadaHiroyuki OsadaChemical Biology Group, RIKEN Center for Sustainable Resource ScienceWakoSaitama351-0198 JapanSearch for other works by this author on:
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CHAPTER 6: Hydrogen Bond Surrogate Stabilized Helices as Protein–Protein Interaction Inhibitorsp124-146ByDaniel Yoo;Daniel YooDepartment of Chemistry, New York University100 Washington Square EastNew YorkNY 10003USA[email protected]Search for other works by this author on:Paramjit S. AroraParamjit S. AroraDepartment of Chemistry, New York University100 Washington Square EastNew YorkNY 10003USA[email protected]Search for other works by this author on:
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CHAPTER 7: Helix-mimetics as Protein–Protein Interaction Inhibitorsp147-170BySiddhartha RoySiddhartha RoySearch for other works by this author on:
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CHAPTER 8: Discovery and Development of Mcl-1 Inhibitors as Anti-cancer Therapeutics: Hit to Clinical Candidate Optimizationp171-208ByKarson J. Kump;Karson J. KumpDepartment of Pathology and Molecular & Cellular Pathology Graduate ProgramAnn ArborMichigan 48109USA[email protected]Program in Chemical BiologyAnn ArborMichigan 48109USASearch for other works by this author on:Zaneta Nikolovska-ColeskaZaneta Nikolovska-ColeskaDepartment of Pathology and Molecular & Cellular Pathology Graduate ProgramAnn ArborMichigan 48109USA[email protected]Program in Chemical BiologyAnn ArborMichigan 48109USAInterdepartmental Graduate Program in Medicinal ChemistryAnn ArborMichigan 48109USARogel Cancer Center, University of Michigan Medical SchoolAnn ArborMichigan 48109USASearch for other works by this author on:
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CHAPTER 9: Pharmacological Regulation and Functional Significance of Chromatin Binding by BET Tandem Bromodomainsp209-248ByMichael D. Olp;Michael D. OlpDepartment of Biochemistry, Medical College of WisconsinMilwaukeeWisconsin 53226USA[email protected]Search for other works by this author on:Brian C. SmithBrian C. SmithDepartment of Biochemistry, Medical College of WisconsinMilwaukeeWisconsin 53226USA[email protected]Search for other works by this author on:
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CHAPTER 10: Small-molecule Modulators of Protein–Protein Interactions: Focus on 14-3-3 PPIsp249-279ByL. Iralde-Lorente;L. Iralde-LorenteDepartment of Biotechnology, Chemistry and Pharmacy, Università degli Studi di SienaSienaItalySearch for other works by this author on:M. Botta;M. BottaDepartment of Biotechnology, Chemistry and Pharmacy, Università degli Studi di SienaSienaItalySearch for other works by this author on:C. OttmannC. OttmannLaboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Technische Universiteit EindhovenDen Dolech 25612 AZ EindhovenThe Netherlands[email protected]Department of Chemistry, University of Duisburg-EssenUniversitätsstraße 745117EssenGermanySearch for other works by this author on:
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CHAPTER 11: Discovery of AMG 232, a Small Molecule MDM2 Inhibitor in Clinical Development and its Back-up Clinical Candidate, AM-7209p280-301ByYosup Rew;Yosup RewFormerly at Amgen Inc.1120 Veterans BoulevardSouth San FranciscoCA94080USASearch for other works by this author on:John EksterowiczJohn EksterowiczFrontier Medicines Corporation151 Oyster Point Blvd.2nd Floor, South San FranciscoCA94080Formerly at Amgen Inc.1120 Veterans BoulevardSouth San FranciscoCA94080USASearch for other works by this author on:
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CHAPTER 12: Small-molecule Inhibitors of Myc–Max Interaction and DNA Bindingp302-338BySteven Fletcher;Steven FletcherDepartment of Pharmaceutical Sciences, University of Maryland School of Medicine20 N Pine Street, N717BaltimoreMD 21201USA[email protected]University of Maryland Greenebaum Cancer CenterBaltimoreMD 21201USASearch for other works by this author on:Edward V. ProchownikEdward V. ProchownikDivision of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, Rangos Research CenterRoom 5124, 4401 Penn AvenuePittsburghPA 15224USA[email protected]The Hillman Comprehensive Cancer Center, UPMCPittsburghUSAThe Department of Microbiology and Molecular Genetics, The University of Pittsburgh School of MedicinePittsburghUSAThe Pittsburgh Liver Research CenterPittsburghUSASearch for other works by this author on:
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CHAPTER 13: Small Molecule Modulators of Endo-lysosomal Toll-like Receptorsp339-372ByArindam Talukdar;Arindam TalukdarDepartment of Organic and Medicinal Chemistry, CSIR-Indian Institute of Chemical Biology4 Raja S. C. Mullick RoadKolkataIndia[email protected]Search for other works by this author on:Ayan Mukherjee;Ayan MukherjeeDepartment of Organic and Medicinal Chemistry, CSIR-Indian Institute of Chemical Biology4 Raja S. C. Mullick RoadKolkataIndia[email protected]Search for other works by this author on:Dipyaman GangulyDipyaman GangulyIICB-Translational Research Unit of Excellence, CSIR-Indian Institute of Chemical BiologyKolkataIndiaSearch for other works by this author on:
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