Nomenclature: LPA5 receptor

Family: Lysophospholipid (LPA) receptors

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 372 12p13.31 LPAR5 lysophosphatidic acid receptor 5
Mouse 7 372 6 Lpar5 lysophosphatidic acid receptor 5
Rat 7 384 4q42 Lpar5 lysophosphatidic acid receptor 5
Previous and Unofficial Names
GPR93
LPAR5
KPG_010
LPA5
lysophosphatidic acid receptor 5
GPR92
G-protein coupled receptor 92
LPAR5 lysophosphatidic acid receptor 5
G protein-coupled receptor 92
LOC500317
RGD1562580
RGD1562580_predicted
similar to Probable G-protein coupled receptor 92
similar to Probable G-protein coupled receptor 92 (predicted)
LOC381810
Gm1072
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
LPA
Comments: Proposed ligand, two publications
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
LPA Hs Full agonist 8.19 pKd 4
pKd 8.19 (Kd 6.4x10-9 M) [4]
alkyl glycerol phosphate 18:1 Rn Full agonist 8.7 pEC50 14
pEC50 8.7 (EC50 2x10-9 M) [14]
farnesyl monophosphate Hs Agonist 7.31 pEC50 14
pEC50 7.31 [14]
farnesyl diphosphate Hs Partial agonist 5.84 – 6.54 pEC50 10,14
pEC50 5.84 – 6.54 (EC50 2.9x10-7 – 1.46x10-6 M) [10,14]
LPA Hs Agonist 4.3 – 7.9 pEC50 8,10,12
pEC50 4.3 – 7.9 [8,10,12]
octyl thiophosphatidic acid Rn Partial agonist 5.68 pEC50 14
pEC50 5.68 (EC50 2.1x10-6 M) [14]
N-arachidonoylglycine Hs Partial agonist <4.3 pEC50 10,14
pEC50 <4.3 (EC50 >5x10-5 M) [10,14]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AM966 Hs Antagonist 5.1 pIC50 13
pIC50 5.1 [13]
AM966 Mm Antagonist 4.6 pIC50 13
pIC50 4.6 [13]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family
G12/G13 family
Other - See Comments
Comments:  Increases cAMP, intracellular calcium, conductance change pathway unknown. Others include: Rho. For a detailed review please see [2].
References:  5
Tissue Distribution
Mast cells, platelets, spleen, heart, small intestine, placenta, colon, liver
Species:  Human
Technique:  Northern blot and RT-PCR
References:  1,9
Small intestine, lung, heart, stomach, colon, spleen, thymus, skin, liver, platelets, mast cells, gastrointestinal lymphocytes, dorsal root ganglia, early embryonic forebrain, rostral midbrain, hindbrain, choroid plexus, embryonic stem cell
Species:  Mouse
Technique:  RT-PCR, in situ hybridisation, IHC
References:  4-5,10-11
Expression Datasets

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays
Receptor internalization
Species:  Rat
Tissue:  Brain
Response measured:  Receptor internalization in B103 neuroblastoma cells
References:  5
Neurite retraction
Species:  Rat
Tissue:  Brain
Response measured:  Neurite retraction in B103 neuroblastoma cells
References:  5
Stress fiber formation
Species:  Rat
Tissue:  Liver
Response measured:  Stress fiber formation in RH7777 hepatoma cells
References:  5
Physiological Functions
Sodium dependent water absorption
Species:  Mouse
Tissue:  Intestine
References:  7
Mediation of neuropathic pain
Species:  Mouse
Tissue:  Spinal chord
References:  6
Release of MIP-1β by mast cells
Species:  Human
Tissue:  Immune
References:  9
Chemorepellent for B16 melanoma cells
Species:  Mouse
Tissue:  Skin
References:  3
Physiological Consequences of Altering Gene Expression
Mice with receptor knockout are protected from partial sciatic nerve ligation-medated neuropathic pain; no baseline phenotype
Species:  Mouse
Tissue:  Spinal cord: dorsal root ganglia and dorsal horn
Technique:  Gene knockouts
References:  6
Available Assays
DiscoveRx PathHunter® CHO-K1 GPR92 β-Arrestin Cell Line (Cat no. 93-0372C2)
PathHunter® eXpress GPR92 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0372E2CP6M)
more info

REFERENCES

1. Amisten S, Braun OO, Bengtsson A, Erlinge D. (2008) Gene expression profiling for the identification of G-protein coupled receptors in human platelets. Thromb. Res.122 (1): 47-57. [PMID:17920662]

2. Choi JW, Herr DR, Noguchi K, Yung YC, Lee CW, Mutoh T, Lin ME, Teo ST, Park KE, Mosley AN, Chun J. (2010) LPA receptors: subtypes and biological actions. Annu. Rev. Pharmacol. Toxicol.50: 157-86. [PMID:20055701]

3. Jongsma M, Matas-Rico E, Rzadkowski A, Jalink K, Moolenaar WH. (2011) LPA is a chemorepellent for B16 melanoma cells: action through the cAMP-elevating LPA5 receptor. PLoS ONE6 (12): e29260. [PMID:22195035]

4. Kotarsky K, Boketoft A, Bristulf J, Nilsson NE, Norberg A, Hansson S, Owman C, Sillard R, Leeb-Lundberg LM, Olde B. (2006) Lysophosphatidic acid binds to and activates GPR92, a G protein-coupled receptor highly expressed in gastrointestinal lymphocytes. J. Pharmacol. Exp. Ther.318 (2): 619-28. [PMID:16651401]

5. Lee CW, Rivera R, Gardell S, Dubin AE, Chun J. (2006) GPR92 as a new G12/13- and Gq-coupled lysophosphatidic acid receptor that increases cAMP, LPA5. J. Biol. Chem.281 (33): 23589-97. [PMID:16774927]

6. Lin ME, Rivera RR, Chun J. (2012) Targeted deletion of LPA5 identifies novel roles for lysophosphatidic acid signaling in development of neuropathic pain. J. Biol. Chem.287 (21): 17608-17. [PMID:22461625]

7. Lin S, Yeruva S, He P, Singh AK, Zhang H, Chen M, Lamprecht G, de Jonge HR, Tse M, Donowitz M, Hogema BM, Chun J, Seidler U, Yun CC. (2010) Lysophosphatidic acid stimulates the intestinal brush border Na(+)/H(+) exchanger 3 and fluid absorption via LPA(5) and NHERF2. Gastroenterology138 (2): 649-58. [PMID:19800338]

8. Lu Y, Wang Z, Li CM, Chen J, Dalton JT, Li W, Miller DD. (2010) Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents. Bioorg. Med. Chem.18 (2): 477-95. [PMID:20056548]

9. Lundequist A, Boyce JA. (2011) LPA5 is abundantly expressed by human mast cells and important for lysophosphatidic acid induced MIP-1β release. PLoS ONE6 (3): e18192. [PMID:21464938]

10. Oh DY, Yoon JM, Moon MJ, Hwang JI, Choe H, Lee JY, Kim JI, Kim S, Rhim H, O'Dell DK, Walker JM, Na HS, Lee MG, Kwon HB, Kim K, Seong JY. (2008) Identification of farnesyl pyrophosphate and N-arachidonylglycine as endogenous ligands for GPR92. J. Biol. Chem.283 (30): 21054-64. [PMID:18499677]

11. Ohuchi H, Hamada A, Matsuda H, Takagi A, Tanaka M, Aoki J, Arai H, Noji S. (2008) Expression patterns of the lysophospholipid receptor genes during mouse early development. Dev. Dyn.237 (11): 3280-94. [PMID:18924241]

12. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen18 (5): 599-609. [PMID:23396314]

13. Swaney JS, Chapman C, Correa LD, Stebbins KJ, Bundey RA, Prodanovich PC, Fagan P, Baccei CS, Santini AM, Hutchinson JH et al.. (2010) A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br. J. Pharmacol.160 (7): 1699-713. [PMID:20649573]

14. Williams JR, Khandoga AL, Goyal P, Fells JI, Perygin DH, Siess W, Parrill AL, Tigyi G, Fujiwara Y. (2009) Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation. J. Biol. Chem.284 (25): 17304-19. [PMID:19366702]

To cite this database page, please use the following:

Yun C. Yung, Jerold Chun, Chido Mpamhanga.
Lysophospholipid (LPA) receptors: LPA5 receptor. Last modified on 24/01/2014. Accessed on 20/08/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=124.

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