Allosteric Modulation of G Protein-Coupled Receptors

Allosteric Modulation of G Protein-Coupled Receptors is a comprehensive book that reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research and discussing key methodologies. It highlights the importance of allosteric modulators in drug discovery and discusses recent advances in our understanding of GPCR signaling mechanisms.

Format: Paperback / softback
Length: 212 pages
Publication date: 10 February 2022
Publisher: Elsevier Science Publishing Co Inc

G protein-coupled receptors (GPCRs) are a class of cell surface receptors that play a crucial role in transmitting signals within cells. They are activated by ligands, such as hormones, neurotransmitters, and other molecules, and they initiate a variety of cellular responses, including hormone secretion, neurotransmitter release, and cell growth.

Allosteric modulation is a mechanism by which GPCRs can be regulated in response to ligand binding. It involves the interaction of ligands with allosteric sites on the receptor, which are located on the receptor's surface or within its transmembrane domain. These allosteric sites are distinct from the orthosteric sites that bind the ligand directly, and they can modulate the receptor's activity in different ways.

One of the key features of allosteric modulation is its ability to fine-tune the receptor's activity. By binding to allosteric sites, ligands can increase or decrease the receptor's affinity for its endogenous ligand, or they can alter the receptor's signaling properties. This can have a significant impact on the cellular response to the ligand, and it allows for a more precise regulation of GPCR function.

There are several different types of allosteric modulators, including agonists, antagonists, and inverse agonists. Agonists bind to allosteric sites and activate the receptor, while antagonists bind to allosteric sites and inhibit the receptor's activity. Inverse agonists bind to allosteric sites and have the opposite effect of agonists, inhibiting the receptor's activity.

GPCRs are also regulated by other mechanisms, such as phosphorylation, dephosphorylation, and internalization. These mechanisms can also modulate the receptor's activity and are often involved in the regulation of GPCR function in response to different environmental cues.

The study of GPCR allosteric modulation has been an active area of research in recent years. This has led to the development of new drugs that target GPCRs, including drugs for the treatment of cardiovascular disease, depression, and other disorders.

In conclusion, G protein-coupled receptors are a class of cell surface receptors that play a crucial role in transmitting signals within cells. Allosteric modulation is a mechanism by which GPCRs can be regulated in response to ligand binding, and it allows for a more precise regulation of GPCR function. The study of GPCR allosteric modulation has led to the development of new drugs that target GPCRs, and it has important implications for the treatment of a variety of disorders.

Weight: 352g
Dimension: 227 x 150 x 18 (mm)
ISBN-13: 9780128197714