Allosterism in Drug Discovery
About this book
Although the concept of allosterism has been known for over half a century, its application in drug discovery has exploded in recent years. The emergence of novel technologies that enable molecular-level ligand-receptor interactions to be studied in studied in unprecedented detail has driven this trend. This book, written by the leaders in this young research area, describes the latest developments in allosterism for drug discovery.
Bringing together research in a diverse range of scientific disciplines, Allosterism in Drug Discovery is a key reference for academics and industrialists interested in understanding allosteric interactions. The book provides an in-depth review of research using small molecules as chemical probes and drug candidates that interact allosterically with proteins of relevance to life sciences and human disease. Knowledge of these interactions can then be applied in the discovery of the novel therapeutics of the future.
This book will be useful for people working in all disciplines associated with drug discovery in academia or industry, as well as postgraduate students who may be working in the design of allosteric modulators.
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Information
Table of contents
- Cover
- Allosterism in Drug Discovery
- Preface
- Dedication
- Contents
- Chapter 1 - Modulation of Biological Targets Using Allosteric Ligands: Food for Thought
- Chapter 2 - Identifying and Quantifying Allosteric Drug Function
- Chapter 3 - Targeting Catalytic and Non-Catalytic Functions of Protein Kinases
- Chapter 4 - Molecular Biology Techniques Applied to GPCR Allosteric and Biased Ligands
- Chapter 5 - Examining Allosterism in a Dimeric G-Protein-Coupled Receptor Context
- Chapter 6 - A Unifying Approach to the Duality of âEnergeticâ Versus âConformationalâ Formulations of Allosteric Coupling: Mechanistic Implications for GPCR Allostery
- Chapter 7 - mGlu2 Receptor Positive Allosteric Modulators
- Chapter 8 - Muscarinic Receptors Allosteric Modulation
- Chapter 9 - Positive Allosteric Modulators of Opioid Receptors
- Chapter 10 - mGlu4 PET Ligands as Enablers of Target Biology Understanding
- Chapter 11 - Allosteric Modulators of Adenosine, P2Y and P2X Receptors
- Chapter 12 - Positive Allosteric Modulators of G-Protein-Coupled Receptors that Act via Covalent Mechanisms of Actionâ
- Chapter 13 - Mechanism of Action of a GluN2C- and GluN2D-Selective NMDA Receptor Positive Allosteric Modulator
- Chapter 14 - Development of AMPA Receptor Modulators as Cognition Enhancers
- Chapter 15 - Allosteric Modulation of Neuronal Nicotinic Acetylcholine Receptors
- Chapter 16 - Allosteric Binding in the Serotonin Transporter â Pharmacology, Structure, Function and Potential Use as a Novel Drug Target
- Chapter 17 - Allosteric Inhibition of Abl Kinase
- Chapter 18 - Allosteric Modulators of Heat Shock Protein 90 (HSP90)
- Subject Index
