From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors

Volume 88 in the Advances in Pharmacology series, edited by Christopher J. Langmead, presents a comprehensive compilation of chapters from leading experts in the field. This updated edition delves into the latest advancements in G protein-coupled receptor (GPCR) research, providing insights into the role of allosteric modulation in various diseases and therapeutic interventions.

Targeting Muscarinic M1 Receptor in Neurodegeneration

This chapter explores the potential of targeting the muscarinic M1 receptor as a therapeutic strategy for neurodegenerative disorders. It discusses the current understanding of the M1 receptor’s role in the nervous system and its potential as a drug target for diseases such as Alzheimer’s and Parkinson’s.

Photo-Switchable Allosteric Ligands

This section introduces the concept of photo-switchable allosteric ligands, which can be controlled by light to modulate GPCR activity. The authors discuss the potential applications of these innovative compounds in basic research and drug development.

Computational Approaches for the Design of mGlu Receptor Allosteric Modulators

This chapter outlines the computational methods used in the design of allosteric modulators for metabotropic glutamate (mGlu) receptors. It covers the challenges and opportunities in using computational tools to identify and optimize potential drug candidates.

Allosteric Modulation of GLP-1 Receptor in Metabolic Disorders

This section focuses on the glucagon-like peptide-1 (GLP-1) receptor, a key player in glucose homeostasis and metabolic regulation. The authors discuss the potential of allosteric modulation of the GLP-1 receptor as a therapeutic approach for treating metabolic disorders such as type 2 diabetes.

Group II mGluR Roles in the Nervous System and Their Roles in Addiction

This chapter delves into the functions of group II mGlu receptors in the nervous system, with a particular emphasis on their involvement in addiction. The authors explore the potential of targeting these receptors for the development of novel treatments for addiction.

RAMPs as Allosteric Modulators of Class B GPCRs

This section discusses the role of receptor activity-modifying proteins (RAMPs) in modulating the activity of class B GPCRs. The authors highlight the potential therapeutic applications of targeting RAMP-GPCR interactions.

Structure-Based Discovery and Development of mGlu5 NAMs

This chapter covers the structure-based approaches used in the discovery and development of negative allosteric modulators (NAMs) for the mGlu5 receptor. It provides insights into the challenges and opportunities in using structural information to design and optimize drug candidates.