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.
Inhaltsverzeichnis
Modulation of Biological Targets: Why Use Allosteric Ligands?; Identifying and Quantifying Allosteric Drug Function; Targeting Catalytic and Non-catalytic Functions of Protein Kinases; Molecular Biology Techniques Applied to GPCR Allosteric and Biased Ligands; Examining Allosterism in a Dimeric GPCR Context; A Unifying Approach to the Duality of ‚Energetic‘ Versus ‚Conformational‘ Formulations of Allosteric Coupling: Mechanistic Implications on GPCR Allostery; m Glu R2 Positive Allosteric Modulators; Muscarinic Receptors Allosteric Modulation; Positive Allosteric Modulators of Opioid Receptors; m Glu R7 allostery: up and down modulation; Allosteric Modulators of Adenosine, P2Y and P2X Receptors; Positive Allosteric Modulators of G Protein-Coupled Receptors that Act via Covalent Mechanisms of Action; m Glu R4 PET ligands as enablers of target biology understanding; Mechanism of action of a Glu N2C- and Glu N2D-selective NMDA receptor positive allosteric modulator; Development of AMPA Receptor Modulators as Cognition Enhancers; Allosteric modulation of the neuronal nicotinic acetylcholine receptor; Allosteric Binding in the Serotonin Transporter – Pharmacology, Structure, Function and Potential Use as a Novel Drug Target; Allosteric Inhibition of Abl Kinase; Allosteric Modulators of Heat Shock Protein 90 (HSP90); A look forward;
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