Page last updated: 2024-10-24

G protein-coupled receptor homodimeric complex

Definition

Target type: cellularcomponent

A protein complex that contains two G protein-coupled receptors (GPCRs) of the same subtype. Formation of a GPCR homodimer may be important for the transport of newly formed receptors to the cell surface, and the function of the receptor. [GOC:al, GOC:bf, PMID:10713101, PMID:16670762]

G protein-coupled receptor (GPCR) homodimers are formed when two identical GPCR molecules associate with each other. This association can occur through various interactions, including transmembrane domain interactions, extracellular loop interactions, and interactions with intracellular signaling proteins. The cellular component of a GPCR homodimer is complex and dynamic, involving multiple cellular structures and processes.

**Plasma Membrane:**
- GPCR homodimers are primarily localized to the plasma membrane, where they are embedded within the lipid bilayer.
- The transmembrane domains of the GPCRs span the membrane, with their extracellular domains exposed to the external environment and their intracellular domains facing the cytoplasm.
- The plasma membrane provides a platform for the interaction of GPCR homodimers with extracellular ligands and intracellular signaling molecules.

**Lipid Rafts:**
- GPCR homodimers are often enriched in lipid rafts, which are specialized microdomains within the plasma membrane.
- Lipid rafts are characterized by their high cholesterol and sphingolipid content, creating a more ordered and rigid environment.
- The association of GPCR homodimers with lipid rafts facilitates their signaling and trafficking.

**Cytoskeleton:**
- The cytoskeleton, a network of protein filaments that provides structural support to cells, plays a role in the localization and signaling of GPCR homodimers.
- GPCR homodimers can interact with cytoskeletal proteins, such as actin and tubulin, which can influence their trafficking and signaling.

**Signal Transduction Complexes:**
- GPCR homodimers often associate with other proteins to form signal transduction complexes.
- These complexes may include G proteins, adaptor proteins, kinases, and phosphatases.
- The formation of these complexes enables the efficient propagation of signals downstream of GPCR activation.

**Intracellular Compartments:**
- In addition to the plasma membrane, GPCR homodimers can also be found in intracellular compartments, such as the endoplasmic reticulum (ER) and Golgi apparatus.
- The ER serves as the site of GPCR synthesis and folding, while the Golgi apparatus is involved in protein sorting and trafficking.
- The trafficking of GPCR homodimers between these compartments can be regulated by various mechanisms.

**Dynamic Nature:**
- The cellular component of a GPCR homodimer is not static but rather dynamic.
- GPCR homodimers can undergo conformational changes upon ligand binding, which can alter their interactions with other cellular components.
- The localization and signaling of GPCR homodimers can be regulated by various cellular processes, including phosphorylation, ubiquitination, and endocytosis.

In summary, the cellular component of a GPCR homodimer is a complex and dynamic entity that involves multiple cellular structures, processes, and interactions. The localization and signaling of GPCR homodimers are regulated by various factors, including lipid rafts, the cytoskeleton, signal transduction complexes, and intracellular trafficking.'
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Proteins (1)

ProteinDefinitionTaxonomy
Metabotropic glutamate receptor 1A metabotropic glutamate receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13255]Homo sapiens (human)

Compounds (49)

CompoundDefinitionClassesRoles
alpha-methyl-4-carboxyphenylglycine
ibotenic acidIbotenic Acid: A neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.non-proteinogenic alpha-amino acidneurotoxin
4-carboxy-3-hydroxyphenylglycine4-carboxy-3-hydroxyphenylglycine: weak agonist at metabotropic glutamate receptors; occludes the action of 1-aminocyclopentyl-1,3-dicarboxylate in hippocampushydroxybenzoic acid
1-aminoindan-1,5-dicarboxylic acid1-aminoindan-1,5-dicarboxylic acid: structure given in first source
4-carboxyphenylglycine4-carboxyphenylglycine: RN given for (+-)-isomer; RN for cpd without isomeric designation not available 3/93; glutamate receptor antagonistalpha-amino acid
aspartic acidaspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent

Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.

L-aspartic acid : The L-enantiomer of aspartic acid.
aspartate family amino acid;
aspartic acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
mouse metabolite;
neurotransmitter
d-glutamateD-alpha-amino acid;
glutamic acid
Escherichia coli metabolite;
mouse metabolite
glutamic acidglutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.

Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
quisqualic acidQuisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.non-proteinogenic alpha-amino acid
1-amino-1,3-dicarboxycyclopentane, (trans)-isomer
d-aspartic acidaspartic acid;
D-alpha-amino acid
mouse metabolite
L-2-aminoadipic acidL-2-aminoadipic acid : The L-enantiomer of 2-aminoadipic acid.2-aminoadipic acidEscherichia coli metabolite;
human metabolite
alpha-aminopimelic acid2-aminopimelic acid : An amino dicarboxylic acid that is heptanedioic acid in which a hydrogen at position 2 is replaced by an amino group. It is a component of the cell wall peptidoglycan of bacteria.

alpha-aminopimelic acid: antagonizes glutamate-induced inhibitions of Helix neurones
amino dicarboxylic acid;
non-proteinogenic alpha-amino acid
bacterial metabolite
1-amino-1,3-dicarboxycyclopentane1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
philanthotoxin 343philanthotoxin 343: structure given in first source (see article's footnote); identical to philanthotoxin 433 except that the number of methylene groups between the respective amine moieties is 3,4,3 instead of 4,3,3N-acyl-amino acid
alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acidalpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid: RN given refers to cpd without isomeric designation; structure given in first source
homocysteic acidhomocysteic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group has benn oxidised to the corresponding sulfonic acid.

homocysteic acid: promotes growth in hypophysectomized rats; RN given refers to parent cpd

L-homocysteic acid : A homocysteic acid with L-configuration.
homocysteic acidNMDA receptor agonist
2-amino-4-phosphonobutyric acid(2S)-2-amino-4-phosphonobutanoic acid : A non-proteinogenc L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. It is a potent and selective agonist for the group III metabotropic glutamate receptors (mGluR4/6/7/8).non-proteinogenic L-alpha-amino acid;
phosphonic acids
metabotropic glutamate receptor agonist
eglumetadeglumetad: LY-354740 is the active isomer, LY-366563 is the inactive isomer, and LY 314582 is the racemate; structure given in first sourceL-alpha-amino acid
3,5-dihydroxyphenylglycine(S)-3,5-dihydroxyphenylglycine : A glycine derivative that is L-alpha-phenylglycine substituted at positions 3 and 5 on the phenyl ring by hydroxy groups.amino acid zwitterion;
non-proteinogenic L-alpha-amino acid;
resorcinols
alpha-methyl-4-carboxyphenylglycine(S)-alpha-methyl-4-carboxyphenylglycine : A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist.

alpha-methyl-4-carboxyphenylglycine: glutamate receptor antagonist
non-proteinogenic alpha-amino acidmetabotropic glutamate receptor antagonist
9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinoneorganic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
4-bromohomoibotenic acid, (rs)-isomer
6-methyl-2-(phenylethynyl)pyridine2-methyl-6-(phenylethynyl)pyridine : A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.

6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist
acetylenic compound;
methylpyridines
anxiolytic drug;
metabotropic glutamate receptor antagonist
4-methylglutamic acid, threo-(l)-isomer
sib 1757SIB 1757: a selective mGluR5 antagonist; structure in first source
l-2-(carboxypropyl)glycine
2-(2,3-dicarboxycyclopropyl)glycine
2r,4r-4-aminopyrrolidine-2,4-dicarboxylatepyrrolidinedicarboxylic acid
upf 596UPF 596: structure in first source
ly-367385
sib 1893SIB 1893: a selective mGluR5 antagonist; structure in first source
4-carboxy-3-hydroxyphenylglycine
1-amino-1,3-dicarboxycyclopentane, cis-(1s,3s)-isomer
ampa, (r)-isomer
1-aminocyclopentane-1,3,4-tricarboxylic acid1-aminocyclopentane-1,3,4-tricarboxylic acid: metabolic glutamate receptor (mGluR) antagonist; structure in first source
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine: an excitatory amino acid antagonist
ly 341495xanthenes
mgs 0028MGS 0028: a group II mGluR agonist; structure in first source
bay36-7620BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. ; structure in first source
ly 389795LY 389795: a group II metabotropic glutamate receptor agonist; structure in first source
ly 379268LY 379268 : An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia.

LY 379268: group II metabotropic glutamate receptor agonist; structure in first source
amino dicarboxylic acid;
bridged compound;
organic heterobicyclic compound
antipsychotic agent;
anxiolytic drug;
metabotropic glutamate receptor agonist;
neuroprotective agent
r 214127R 214127: an mGlu1 receptor ligand; structure in first source
jnj16259685organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
a 794282
a-841720A-841720: structure in first source
sp 2033-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile: a radioligand for mGlu5 receptor; structure in first source
fenobamfenobam: in USAN fenobam refers to monohydrateureas