Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Selected 3D Structures
- Natural/Endogenous Ligands
- Rank order lists
- Agonists
- Antagonists
- Allosteric Modulators
- Immuno Cell Type Associations
- Transduction Mechanisms
- Tissue Distribution
- Expression Datasets
- Functional Assays
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- General Comments
- References
- Contributors
- How to cite this page
Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 378 | 9q22.1 | S1PR3 | sphingosine-1-phosphate receptor 3 | |
| Mouse | 7 | 378 | 13 A5 | S1pr3 | sphingosine-1-phosphate receptor 3 | |
| Rat | 7 | 379 | 17 p14 | S1pr3 | sphingosine-1-phosphate receptor 3 | |
| Previous and Unofficial Names |
| edg3 | endothelial differentiation G protein-coupled receptor 3 |
| Database Links |
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| Specialist databases | |
| GPCRdb | s1pr3_human (Hs), s1pr3_mouse (Mm) |
| Other databases | |
| Alphafold | Q99500 (Hs), Q9Z0U9 (Mm) |
| ChEMBL Target | CHEMBL3892 (Hs) |
| Ensembl Gene | ENSG00000213694 (Hs), ENSMUSG00000067586 (Mm), ENSRNOG00000014524 (Rn) |
| Entrez Gene | 1903 (Hs), 13610 (Mm), 306792 (Rn) |
| Human Protein Atlas | ENSG00000213694 (Hs) |
| KEGG Gene | hsa:1903 (Hs), mmu:13610 (Mm), rno:306792 (Rn) |
| OMIM | 601965 (Hs) |
| Pharos | Q99500 (Hs) |
| RefSeq Nucleotide | NM_005226 (Hs), NM_010101 (Mm) |
| RefSeq Protein | NP_005217 (Hs), NP_034231 (Mm) |
| UniProtKB | Q99500 (Hs), Q9Z0U9 (Mm) |
| Wikipedia | S1PR3 (Hs) |
| Selected 3D Structures |
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| Natural/Endogenous Ligands |
| dihydrosphingosine 1-phosphate |
| sphingosine 1-phosphate |
| sphingosylphosphorylcholine |
| Comments: Sphingosine 1-phosphate exhibits greater potency than sphingosylphosphorylcholine |
| Potency order of endogenous ligands |
| sphingosine 1-phosphate > dihydrosphingosine 1-phosphate [35] |
Download all structure-activity data for this target as a CSV file 
| Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific agonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| BML-241 (or also known as CAY10444) has been reported and widely used as S1P3 antagonist, while its potency and selectivity is equivocal [25]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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| Cell Type Associations | ||||||||
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
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Gi/Go family Gq/G11 family G12/G13 family |
Adenylyl cyclase inhibition Phospholipase C stimulation |
| Comments: Activation of MAPK [36] and Akt [5-6]. | |
| References: 2,47 | |
| Tissue Distribution
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| Expression Datasets |
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| Functional Assays
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| Physiological Consequences of Altering Gene Expression
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| Phenotypes, Alleles and Disease Models
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Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| General Comments |
| Hill et al. (2018) report on studies that show the involvement of S1PR3 in the generation of pain and itch [19]. They conclude that S1PR3 acts through TRPV1 channels (αq/PLC/PIP2 cleavage dependent) in heat nociceptors to mediate pain sensation, and through TRPA1 channels (βγ subunit dependent) in pruriceptors to mediate itch, and that identifying the role played by S1PR3 in these sensations paves the way for the development of S1PR3 modulators for managing pain and itch. |
References
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