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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...

Transducer Mechanism: G Protein–Coupled Receptors

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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,...

Protein-protein Interfaces

Protein-protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...

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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.

Assembly of Signaling Complexes

Assembly of Signaling Complexes

Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
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Related Experiment Video

Updated: Dec 27, 2025

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

Published on: March 16, 2020

DIMERBOW: exploring possible GPCR dimer interfaces.

Adrián García-Recio¹, Gemma Navarro^2,3, Rafael Franco^3,4

¹Laboratori de Medicina Computacional, Unitat de Bioestadistica, Facultat de Medicina, Universitat Autònoma de Barcelona, Bellaterra 08193, Spain.

Bioinformatics (Oxford, England)

|February 26, 2020

Summary

This summary is machine-generated.

G protein-coupled receptors (GPCRs) form complexes with unique functions. DIMERBOW visualizes potential GPCR dimers in solved structures, aiding in modeling GPCR homomers.

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Last Updated: Dec 27, 2025

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Published on: March 16, 2020

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Area of Science:

Biochemistry
Structural Biology
Pharmacology

Background:

G protein-coupled receptors (GPCRs) can form homo-, heterodimers, and higher-order oligomers, exhibiting distinct functions compared to their monomeric forms.
Understanding the quaternary structure and type of complex formed by GPCRs is crucial for unlocking their pharmacological potential, but current information is limited.

Purpose of the Study:

To present DIMERBOW, a novel database and web application for exploring potential GPCR dimers.
To facilitate the identification of suitable structural templates for modeling GPCR homomers.

Main Methods:

Development of a database and web application (DIMERBOW).
Visual browsing of the complete repertoire of potential GPCR dimers within solved structures.

Main Results:

DIMERBOW provides a comprehensive resource for visualizing GPCR dimer interfaces from existing structural data.
The tool assists researchers in identifying potential GPCR homodimers and heterodimers.

Conclusions:

DIMERBOW enhances the study of GPCR oligomerization by providing visual access to potential dimeric complexes.
This resource supports the structural modeling of GPCR homomers, advancing GPCR pharmacology research.