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 UTP. [GOC:mah]
G protein-coupled UTP receptors (UTP-GPCRs) are integral membrane proteins that mediate cellular responses to the nucleotide uridine triphosphate (UTP). These receptors are involved in a wide range of physiological processes, including inflammation, cell proliferation, and smooth muscle contraction.
The molecular function of UTP-GPCR activity involves a complex interplay of events that ultimately leads to the activation of downstream signaling pathways.
1. **Ligand Binding:** UTP binds to the extracellular domain of the receptor, triggering a conformational change in the protein.
2. **G Protein Activation:** This conformational change activates a heterotrimeric G protein, which is composed of alpha, beta, and gamma subunits. The alpha subunit is bound to GDP in its inactive state. Upon receptor activation, the alpha subunit exchanges GDP for GTP, becoming activated.
3. **Signaling Cascade Initiation:** The activated alpha subunit dissociates from the beta and gamma subunits and interacts with downstream effector molecules, such as phospholipase C (PLC).
4. **Second Messenger Production:** PLC catalyzes the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) into diacylglycerol (DAG) and inositol trisphosphate (IP3). These second messengers activate protein kinase C (PKC) and release calcium from intracellular stores, respectively.
5. **Cellular Response:** The activation of PKC and calcium signaling pathways leads to a variety of cellular responses, including the activation of transcription factors, the regulation of gene expression, and the modulation of cell morphology and function.
6. **Desensitization:** Prolonged exposure to UTP can lead to receptor desensitization, a process that limits the duration of the cellular response. Desensitization involves the phosphorylation of the receptor, which reduces its affinity for UTP and inhibits its ability to activate G proteins.
In summary, UTP-GPCR activity involves a series of events, starting with ligand binding and culminating in the activation of downstream signaling pathways. These signaling pathways ultimately lead to a diverse array of cellular responses, highlighting the importance of UTP-GPCRs in cellular regulation and physiological processes.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| P2Y purinoceptor 2 | A P2Y purinoceptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41231] | Homo sapiens (human) |
| P2Y purinoceptor 6 | A P2Y purinoceptor 6 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15077] | Homo sapiens (human) |
| P2Y purinoceptor 4 | A P2Y purinoceptor 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P51582] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid | 5'-phosphopyridoxal-6-azobenzene-2,4-disulfonic acid : An arenesulfonic acid that is pyridoxal 5'-phosphate carrying an additional 2,4-disulfophenylazo substituent at position 6. pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid: a novel antagonist that selectively blocks P2 purinoceptor receptors; a useful tool to study co-transmission in tissues when ATP and coexisting neurotransmitters act in concert | arenesulfonic acid; azobenzenes; methylpyridines; monohydroxypyridine; organic phosphate; pyridinecarbaldehyde | purinergic receptor P2X antagonist |
| suramin | suramin : 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 diphosphate | Adenosine 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 diphosphate | Uridine 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 |
| adenosine monophosphate | Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position. | adenosine 5'-phosphate; purine ribonucleoside 5'-monophosphate | adenosine A1 receptor agonist; cofactor; EC 3.1.3.1 (alkaline phosphatase) inhibitor; EC 3.1.3.11 (fructose-bisphosphatase) inhibitor; fundamental metabolite; micronutrient; nutraceutical |
| cytidine diphosphate | Cytidine 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 triphosphate | Uridine 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 |
| cytidine triphosphate | Cytidine Triphosphate: Cytidine 5'-(tetrahydrogen triphosphate). A cytosine nucleotide containing three phosphate groups esterified to the sugar moiety. | cytidine 5'-phosphate; pyrimidine ribonucleoside 5'-triphosphate | Escherichia coli metabolite; mouse metabolite |
| trypan blue | VisionBlue: A trypan blue ophthalmic solution. | ||
| suramin sodium | suramin sodium : An organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness. | organic sodium salt | 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 |
| uridine diphosphate glucose | UDP-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-glucose | fundamental metabolite |
| diadenosine tetraphosphate | P(1),P(4)-bis(5'-adenosyl) tetraphosphate : A diadenosyl tetraphosphate compound having the two 5'-adenosyl residues attached at the P(1)- and P(4)-positions. | diadenosyl tetraphosphate | Escherichia coli metabolite; mouse metabolite |
| deoxyuridine triphosphate | deoxyuridine phosphate; pyrimidine 2'-deoxyribonucleoside 5'-triphosphate | Arabidopsis thaliana metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite | |
| methylthio-adp | |||
| diquafosol | diquafosol: 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 | |||
| 2-chloro-atp | 2-chloro-ATP: new ATP analog; relaxes mammalian gut preparations; structure | ||
| uridine 5'-tetraphosphate | |||
| adenosine 5'-o-(3-thiotriphosphate) | adenosine 5'-[gamma-thio]triphosphate : A nucleoside triphosphate analogue that is ATP in which one of the oxygens attached to 3-phosphate group is replaced by sulfur. adenosine 5'-O-(3-thiotriphosphate): RN given refers to cpd with unspecified locant for thio group; see also records for 1-thio & 2-thio-isomers | nucleoside triphosphate analogue | |
| TTP | pyrimidine ribonucleoside 5'-triphosphate | ||
| 4-thiouridine triphosphate | |||
| 2-methylthio-atp | 2-methylthio-ATP: purinergic receptors agonist; relaxes mammalian gut preparations; structure given in first source | ||
| 5-bromouridine triphosphate | 5-bromouridine 5'-triphosphate : A pyrimidine ribonucleoside 5'-triphosphate having 5-bromouracil as the pyrimidine component. | organobromine compound; pyrimidine ribonucleoside 5'-triphosphate | |
| denufosol tetrasodium | |||
| denufosol tetrasodium | denufosol tetrasodium: for treatment of cystic fibrosis | ||
| 5-fluorouridine 5'-triphosphate | |||
| a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
| 4-thiouridylic acid | |||
| acid blue 40 | Acid Blue 40: a textile dye; structure in first source | ||
| acid blue 25 | |||
| guanosine diphosphate | Guanosine 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 |