Targeting Protein-Protein Interactions by Small Molecules

Description

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. Front Matter ....Pages i-xi Front Matter ....Pages 1-1 Overview of Protein-Protein Interactions and Small-Molecule Inhibitors Under Clinical Development (Guoqiang Dong, Chunquan Sheng)....Pages 3-28 High-Throughput Screening in the Discovery of Small-Molecule Inhibitors of Protein-Protein Interactions (Chunlin Zhuang, Chunquan Sheng)....Pages 29-51 Hot Spot-Based Design of Small-Molecule Inhibitors for Protein-Protein Interactions (Haitao Ji)....Pages 53-71 Computational Methods Applicable to the Discovery of Small-Molecule Inhibitors of Protein-Protein Interactions (Li Han, Renxiao Wang)....Pages 73-94 Experimental Methods Used for Identifying Small-Molecule Inhibitors of Protein-Protein Interaction (Mi Zhou, Qing Li, Wenna Kong, Renxiao Wang)....Pages 95-133 Fragment-Based Drug Discovery for Developing Inhibitors of Protein-Protein Interactions (Bing Xiong, Qi Wang, Jingkang Shen)....Pages 135-176 Front Matter ....Pages 177-177 Small Molecule Inhibitors Targeting New Targets of Protein-Protein Interactions (Liyan Yue, Wei Wan, Pan Xu, Linjuan Li, Chen Wang, Yuanyuan Zhang et al.)....Pages 179-211 The Development of New Spirooxindoles Targeting the p53–MDM2 Protein-Protein Interactions for Cancer Therapy (Bin Yu, Hong-Min Liu)....Pages 213-237 Small-Molecule Inhibitors for the β-Catenin/T Cell Factor Protein-Protein Interaction (Yongqiang Zhang, Wei Wang)....Pages 239-248 Discovery and Development of Keap1-Nrf2 Protein-Protein Interaction Inhibitors (Zhengyu Jiang, Qidong You)....Pages 249-286 BRDT Inhibitors for Male Contraceptive Drug Discovery: Current Status (Zhenyuan Miao, Xianghong Guan, Jiewei Jiang, Gunda I. Georg)....Pages 287-315 Targeting Protein-Protein Interactions in Small GTPases (Jiahui Liu, Ning Kang, Yaxue Zhao, Mingyan Zhu)....Pages 317-329