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G protein-coupled UDP receptor activity

Definition

Target type: molecularfunction

Combining with a nucleotide and transmitting the signal to a heterotrimeric G-protein complex to initiate a change in cell activity, activated by UDP. [GOC:mah]

G protein-coupled UDP receptors (GPCRs) are integral membrane proteins that play a crucial role in cellular signaling. These receptors bind UDP, a ubiquitous nucleotide, and initiate downstream signaling cascades through the activation of G proteins. The molecular function of G protein-coupled UDP receptor activity can be described in several key steps:

1. **Ligand Binding:** UDP binds to the extracellular domain of the receptor, triggering a conformational change in the protein. This conformational change is essential for the subsequent activation of G proteins.

2. **G Protein Coupling:** Upon UDP binding, the receptor interacts with and activates heterotrimeric G proteins. These proteins are composed of three subunits: alpha (α), beta (β), and gamma (γ). The α subunit is responsible for binding GDP in its inactive state.

3. **GDP/GTP Exchange:** The activated receptor facilitates the exchange of GDP for GTP on the α subunit of the G protein. This exchange event marks the activation of the α subunit, which subsequently dissociates from the βγ subunits.

4. **Signal Transduction:** The activated α subunit, bound to GTP, interacts with downstream effector proteins, such as adenylyl cyclase, phospholipase C, or ion channels. This interaction initiates a cascade of intracellular signaling events, leading to diverse cellular responses.

5. **GTP Hydrolysis and Deactivation:** The α subunit has intrinsic GTPase activity, which eventually hydrolyzes GTP to GDP. This hydrolysis event inactivates the α subunit, allowing it to reassociate with the βγ subunits and return the G protein to its inactive state.

6. **Receptor Desensitization:** After prolonged exposure to UDP, the receptor can undergo desensitization, reducing its signaling activity. This desensitization mechanism involves phosphorylation of the receptor by kinases and the binding of arrestin proteins.

In summary, the molecular function of G protein-coupled UDP receptor activity involves a series of events, from ligand binding to signal transduction and deactivation, ultimately leading to the modulation of cellular processes. This intricate signaling pathway plays a vital role in various physiological functions, including inflammation, immune responses, and neuronal activity.'
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Proteins (2)

ProteinDefinitionTaxonomy
P2Y purinoceptor 14A P2Y purinoceptor 14 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15391]Homo sapiens (human)
P2Y purinoceptor 6A P2Y purinoceptor 6 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15077]Homo sapiens (human)

Compounds (19)

CompoundDefinitionClassesRoles
suraminsuramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.

Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
naphthalenesulfonic acid;
phenylureas;
secondary carboxamide
angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
adenosine diphosphateAdenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
fundamental metabolite;
human metabolite
uridine diphosphateUridine Diphosphate: A uracil nucleotide containing a pyrophosphate group esterified to C5 of the sugar moiety.pyrimidine ribonucleoside 5'-diphosphate;
uridine 5'-phosphate
Escherichia coli metabolite;
mouse metabolite
cytidine diphosphateCytidine Diphosphate: Cytidine 5'-(trihydrogen diphosphate). A cytosine nucleotide containing two phosphate groups esterified to the sugar moiety. Synonyms: CRPP; cytidine pyrophosphate.cytidine 5'-phosphate;
pyrimidine ribonucleoside 5'-diphosphate
Escherichia coli metabolite;
mouse metabolite
uridine triphosphateUridine Triphosphate: Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.pyrimidine ribonucleoside 5'-triphosphate;
uridine 5'-phosphate
Escherichia coli metabolite;
mouse metabolite
uridine diphosphate glucoseUDP-alpha-D-glucose : The alpha-anomer of UDP-alpha-D-glucose. It is used in nucleotide sugars metabolism.

Uridine Diphosphate Glucose: A key intermediate in carbohydrate metabolism. Serves as a precursor of glycogen, can be metabolized into UDPgalactose and UDPglucuronic acid which can then be incorporated into polysaccharides as galactose and glucuronic acid. Also serves as a precursor of sucrose lipopolysaccharides, and glycosphingolipids.
UDP-D-glucosefundamental metabolite
uridine diphosphate glucuronic acidUDP-alpha-D-glucuronic acid : A UDP-sugar having alpha-D-glucuronic acid as the sugar component.

Uridine Diphosphate Glucuronic Acid: A nucleoside diphosphate sugar which serves as a source of glucuronic acid for polysaccharide biosynthesis. It may also be epimerized to UDP iduronic acid, which donates iduronic acid to polysaccharides. In animals, UDP glucuronic acid is used for formation of many glucosiduronides with various aglycones.
UDP-D-glucuronic acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
uridine diphosphate galactoseUDP-alpha-D-galactose : A UDP-D-galactose in which the anomeric centre of the galactose moiety has alpha-configuration.

Uridine Diphosphate Galactose: A nucleoside diphosphate sugar which can be epimerized into UDPglucose for entry into the mainstream of carbohydrate metabolism. Serves as a source of galactose in the synthesis of lipopolysaccharides, cerebrosides, and lactose.
UDP-D-galactosemouse metabolite
diquafosoldiquafosol: purinoceptor P2Y(2) receptor agonist

P(1),P(4)-bis(uridin-5'-yl) tetraphosphate : A pyrimidine ribonucleoside 5'-tetraphosphate compound having 5'-uridinyl residues at the P(1)- and P(4)-positions.
pyrimidine ribonucleoside 5'-tetraphosphate;
uridine 5'-phosphate
mouse metabolite;
P2Y2 receptor agonist
phosphoribofuranosylbarbituric acid
uridine 5'-tetraphosphate
TTPpyrimidine ribonucleoside 5'-triphosphate
2-methylthio-atp2-methylthio-ATP: purinergic receptors agonist; relaxes mammalian gut preparations; structure given in first source
5-bromouridine triphosphate5-bromouridine 5'-triphosphate : A pyrimidine ribonucleoside 5'-triphosphate having 5-bromouracil as the pyrimidine component.organobromine compound;
pyrimidine ribonucleoside 5'-triphosphate
denufosol tetrasodium
denufosol tetrasodiumdenufosol tetrasodium: for treatment of cystic fibrosis
4-thiouridylic acid
acid blue 25
guanosine diphosphateGuanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.guanosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor