Title:	Targeting Protein-Protein Interactions by Small Molecules
Authors:	Sheng, Chunquan Georg, Gunda I.
Keywords:	Molecules
Issue Date:	2018
Publisher:	Springer Nature Singapore Pte Ltd.
Description:	Protein-protein interactions (PPIs) regulate a number of biological processes both in normal and disease states, providing a rich source of drug targets for the development of new generation of clinical therapeutics. However, the discovery and development of selective and drug-like small-molecule inhibitors are rather challenging as compared to traditional targets, due to large, flat, and hydrophobic features of the PPI interfaces. Despite the challenges, important progress has been made in the design strategies and clinical development of small-molecule PPI inhibitors. In recent years, with better understanding of the structural biology of PPIs, particularly the “hot spots” as critical interaction components for inhibitor design, the identi fi cation of drug-like PPIs inhibitors has been greatly accelerated. The development of PPI inhibitors as novel therapeutics is coming into reality. Bcl-2 inhibitor venetoclax and LFA-1/ICAM-1 inhibitor li fi tegrast have been approved by the US FDA for clinical use, and a number of other small-molecule PPI inhibitors are currently under clinical evaluation. To summarize recent advances and guide future research, this book will comprehensively introduce state-of-the-art strategies of PPI-based drug discovery focusing on the developments of new methodologies. Moreover, representative case studies will illustrate how these technologies are applied in the discovery of small-molecule PPI inhibitors.
URI:	http://10.6.20.12:80/handle/123456789/75930
ISBN:	978-981-13-0773-7
Appears in Collections:	Chemistry

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