G protein-coupled receptor heterodimeric complex

Definition

Target type: cellularcomponent

A protein complex that contains two G protein-coupled receptors (GPCRs) of different subtypes. Formation of a GPCR heterodimer may alter the functional property of the GPCR. [GOC:al, GOC:bf, PMID:16109836, PMID:20150590]

G protein-coupled receptor (GPCR) heterodimeric complexes are intricate assemblies of two or more GPCRs that associate to form functional units. These complexes display unique signaling properties compared to their individual components, often exhibiting altered ligand binding, signaling pathways, and cellular responses. Their cellular component can be described as follows:

* **Plasma Membrane Localization:** GPCR heterodimers are primarily localized to the plasma membrane, the outermost layer of the cell. This membrane location is crucial for their function as they interact with extracellular ligands to initiate intracellular signaling cascades.

* **Transmembrane Domain Association:** The association between GPCRs within a heterodimer often involves interactions between their transmembrane domains, which are regions spanning the cell membrane. These interactions are mediated by hydrophobic residues, hydrogen bonds, and other non-covalent forces.

* **Cytoplasmic Domain Interactions:** In addition to transmembrane domain interactions, cytoplasmic domains of GPCR heterodimers can also interact with each other or with other intracellular proteins. These interactions contribute to the stability and signaling properties of the complex.

* **Scaffolding Proteins:** Scaffolding proteins can play a significant role in the formation and regulation of GPCR heterodimers. These proteins bind to specific regions of the GPCRs, facilitating their assembly and influencing their signaling activities.

* **Heteromerization Interfaces:** The interfaces where GPCRs interact within a heterodimer are often defined by specific amino acid residues and structural features. These interfaces contribute to the specificity and stability of the complex.

* **Dynamic Nature:** GPCR heterodimerization is often a dynamic process, with complexes forming and dissociating in response to various stimuli. This dynamic nature allows for flexible signaling and adaptation to changing cellular environments.

* **Regulation of Heterodimerization:** The formation and stability of GPCR heterodimers can be regulated by factors such as ligand binding, phosphorylation, and interactions with other proteins.

The cellular component of GPCR heterodimers is thus a complex interplay of membrane localization, transmembrane and cytoplasmic domain interactions, scaffolding proteins, heteromerization interfaces, and dynamic regulation. This intricate architecture enables the unique signaling properties of these multi-component complexes, which are critical for a wide range of cellular processes.'
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Proteins (2)

Compounds (13)