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This book comprehensively reviews the state-of-the-art strategies developed for protein-protein interaction (PPI) inhibitors, and highlights the success stories in new drug discovery and development. Consisting of two parts with twelve chapters, it demonstrates the design strategies and case studies of small molecule PPI inhibitors. The first part discusses various discovery strategies for small molecule PPI inhibitors, such as high throughput screening, hot spot-based design, computational approaches, and fragment-based design. The second part presents recent advances in small molecule inhibitors, focusing on clinical candidates and new PPI targets. This book has broad appeal and is of significant interest to the pharmaceutical science and medicinal chemistry communities.
Sommario
Part 1 Current strategies for the discovery of small-molecule inhibitors of protein-protein interactions.- Overview of Protein-protein Interactions and Small Molecule Inhibitors under Clinical Development.- High throughput screening in the discovery of small molecule inhibitors of protein-protein interactions.- Hot Spot-Based Design of Small-Molecule Inhibitors for Protein-Protein Interactions.- Computational Methods Applicable to the Discovery of Small-Molecule Inhibitors of Protein-Protein Interactions.- Experimental Methods Used for Identifying Small-Molecule Inhibitors of Protein-protein Interaction.- Fragment-based Drug Discovery for Developing Inhibitors of Protein-protein Interactions.- Part 2 Case studies of small-molecule inhibitors of protein-protein interactions.- Small molecule inhibitors targeting new targets of protein-protein interactions.- The Development of New Spirooxindoles Targeting the p53-MDM2 Protein-Protein Interactions for Cancer Therapy.- Small-Molecule Inhibitors for the beta-Catenin/T-Cell Factor Protein-Protein Interaction.- Discovery and development of Keap1-Nrf2 protein-protein interaction inhibitors.- BRDT Inhibitors for Male Contraceptive Drug Discovery: Current Status.- Targeting Protein-Protein Interactions in Small GTPases.
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Chunquan Sheng is currently a Professor, Vice Dean of the School of Pharmacy and the Director of the Department of Medicinal Chemistry at Second Military Medical University (SMMU), P. R. China. He received his PhD degree in Medicinal Chemistry (2005) from SMMU and then worked at the Department of Medicinal Chemistry, School of Pharmacy at SMMU. His research interests include structure-based design and synthesis of drug-like molecules with an emphasis on small molecule inhibitors of protein–protein interactions and multi-targeting drugs. He has published more than 100 research articles and invited reviews in prestigious journals in the field of medicinal chemistry and holds more than 10 patents. He was supported by several programs, including the National Outstanding Young Scholarship from the National Natural Science Foundation of China (NSFC).
Gunda I. Georg is Professor and Head of the Department of Medicinal Chemistry and the founding Director of the Institute for Therapeutics Discovery and Development (ITDD) at the University of Minnesota College of Pharmacy. She holds the Robert Vince Endowed Chair and the McKnight Presidential Chair in Medicinal Chemistry. She is the Co-Editor-in-Chief of the Journal of Medicinal Chemistry, the most cited journal in the field. Dr. Georg received a BS in Pharmacy (1975) and a PhD degree in Medicinal Chemistry (1980) from the Philipps University of Marburg, Germany. She was a postdoctoral fellow at the Department of Chemistry at the University of Ottawa in Canada. After 22 years as a faculty member at the University of Kansas, she joined the University of Minnesota in 2007. Her research focuses on the design, synthesis, and evaluation of biologically active agents.
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