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G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

G Protein-coupled Receptors

G Protein-coupled Receptors

Transducer Mechanism: G Protein–Coupled Receptors

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...

GPCRs Regulate Adenylyl Cylase Activity

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...

G-protein Coupled Receptors

G-protein Coupled Receptors

G-protein Coupled Receptors

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.

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Related Experiment Video

Updated: Mar 14, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Gut hormone GPCRs: structure, function, drug discovery.

Arnau Cordomí¹, Daniel Fourmy², Irina G Tikhonova³

¹Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, Barcelona, Spain.

Current Opinion in Pharmacology

|September 20, 2016

Summary

This summary is machine-generated.

Structural biology advances, like determining the beta2-adrenergic receptor structure, enable understanding receptor-ligand interactions. This facilitates the rational design of new drugs targeting various receptors, including gut hormones.

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Last Updated: Mar 14, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors GPCRs

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Area of Science:

Structural Biology
Molecular Endocrinology
Pharmacology

Background:

High-resolution structures of G protein-coupled receptors (GPCRs) like the beta2-adrenergic receptor have been determined.
Previous structural studies have advanced the understanding of receptor-ligand interactions and structure-activity relationships.
These insights support structure-based drug design for predictable ligand activity.

Purpose of the Study:

To highlight the significance of recent structural biology breakthroughs in understanding receptor function.
To emphasize the potential of structure-based approaches for designing novel therapeutic agents.
To underscore the ongoing challenges and future promise in elucidating gut hormone receptor structures.

Main Methods:

X-ray crystallography for high-resolution structure determination.
Biochemical and biophysical assays for characterizing receptor-ligand interactions.
Computational modeling for structure-based drug design.

Main Results:

Determination of the 3D structure of the beta2-adrenergic receptor in 2007.
Elucidation of structures for other key receptors, including neurotensin and glucagon receptors.
Established framework for understanding structure-activity relationships.

Conclusions:

Structural insights into receptors are revolutionizing drug discovery and development.
Elucidating gut hormone receptor structures in complex with ligands and signaling proteins is a critical future challenge.
This research area holds immense promise for transforming gut hormone endocrinology and therapeutics.