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LPA2 receptor

Family: Lysophospholipid (LPA) receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Expression Datasets
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 351 19p12 LPAR2 lysophosphatidic acid receptor 2
Mouse 7 348 8 B3.3 Lpar2 lysophosphatidic acid receptor 2
Rat 7 265 16p14 Lpar2 lysophosphatidic acid receptor 2
Previous and Unofficial Names
Edg4
lp A2
EDG-4
LPA2
endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor, 4
LOC498609
Pbx4
Pbx4_predicted
RGD1561336
RGD1561336_predicted
endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor 4
lysophosphatidic acid receptor 2
pre-B-cell leukemia transcription factor 4
pre-B-cell leukemia transcription factor 4 (predicted)
similar to endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor 4
similar to endothelial differentiation, lysophosphatidic acid G-protein-coupled receptor 4 (predicted)
Database Links
ChEMBL Target 10814 (Hs)
Ensembl ENSG00000064547 (Hs), ENSMUSG00000031861 (Mm), ENSRNOG00000010758 (Rn)
Entrez Gene 9170 (Hs), 53978 (Mm), 498609 (Rn)
GeneCards LPAR2 (Hs)
GenitoUrinary Development Molecular Anatomy Project Lpar2 (Mm)
HomoloGene 3465 (Hs)
Human Protein Reference Database 05487 (Hs)
InterPro Q9HBW0 (Hs), Q9JL06 (Mm)
KEGG Gene hsa:9170 (Hs), mmu:53978 (Mm), rno:498609 (Rn)
OMIM 605110 (Hs)
PharmGKB Gene PA162394202 (Hs)
PhosphoSitePlus Q9HBW0 (Hs), Q9JL06 (Mm)
Protein Ontology (PRO) PRO:000001685 (Hs)
RefSeq Nucleotide NM_004720 (Hs), NM_020028 (Mm), NM_001109109 (Rn)
RefSeq Protein NP_004711 (Hs), NP_064412 (Mm), NP_001102579 (Rn)
TreeFam ENSG00000064547 (Hs), ENSMUSG00000031861 (Mm), ENSRNOG00000010758 (Rn)
UniGene Hs. 122575 (Hs)
UniProt Q9HBW0 (Hs), Q9JL06 (Mm)
Wikipedia LPA2 receptor
Lysophospholipid (LPA) receptors
Search for 3D structures on the PDB
Search by keyword: Lysophospholipid (LPA) receptors LPA2 receptor Search by accession number: Q9HBW0, Q9JL06
Natural/Endogenous Ligand(s)
LPA
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
2-oleoyl-LPA Hs Agonist 8.0 pEC50 1
LPA Hs Agonist 6.71 – 8.16 pEC50 4,6
dodecylphosphonic acid Hs Full agonist 6.2 pEC50 8
decyl dihydrogen phosphate Hs Full agonist 5.4 pEC50 8
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
Ki16425 Hs Antagonist 5.25 pKi 5
farnesyl monophosphate ? Antagonist 6.8 pIC50 9
AM966 Hs Antagonist 5.8 pIC50 7
farnesyl diphosphate Hs Antagonist 5.68 pIC50 9
AM966 Mm Antagonist 4.6 pIC50 7
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
Gq/G11 family
G12/G13 family 		Adenylate cyclase inhibition
Phospholipase C stimulation
Comments:  Others include: Phosphatidylinositol-3-Kinase, RAS, Rho. For a detailed review please see [2]
References: 
Expression Datasets

Click here to show/hide data

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]

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Physiological Consequences of Altering Gene Expression
No obvious phenotypes, but a decrease in PLC activation is observed
Species:  Mouse
Tissue: 
Technique:  Gene targeting:- replacement vector , deletion of half of exon 2
References:  3
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
D3Bwg0562etm1Roni|Lpar2tm1Jch D3Bwg0562etm1Roni/D3Bwg0562etm1Roni,Lpar2tm1Jch/Lpar2tm1Jch
involves: 129P2/OlaHsd * 129S1/Sv * 129X1/SvJ * C57BL/6		 MGI:106530  MGI:1858422  MP:0004753 abnormal miniature excitatory postsynaptic currents PMID: 19766573 
Lpar2tm1Jch Lpar2tm1Jch/Lpar2tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6		 MGI:1858422  MP:0002169 no abnormal phenotype detected PMID: 12215548 

REFERENCES

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1. Bandoh, K; Aoki, J; Taira, A; Tsujimoto, M; Arai, H; Inoue, K. (2000) Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors. FEBS Lett., 478 (1-2): 159-65. [PMID:10922489]

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. Contos, JJ; Fukushima, N; Weiner, JA; Kaushal, D; Chun, J. (2000) Requirement for the lpA1 lysophosphatidic acid receptor gene in normal suckling behavior. Proc. Natl. Acad. Sci. U.S.A., 97 (24): 13384-9. [PMID:11087877]

4. Im, DS; Heise, CE; Harding, MA; George, SR; O'Dowd, BF; Theodorescu, D; Lynch, KR. (2000) Molecular cloning and characterization of a lysophosphatidic acid receptor, Edg-7, expressed in prostate. Mol. Pharmacol., 57 (4): 753-9. [PMID:10727522]

5. Ohta, H; Sato, K; Murata, N; Damirin, A; Malchinkhuu, E; Kon, J; Kimura, T; Tobo, M; Yamazaki, Y; Watanabe, T; Yagi, M; Sato, M; Suzuki, R; Murooka, H; Sakai, T; Nishitoba, T; Im, DS; Nochi, H; Tamoto, K; Tomura, H; Okajima, F. (2003) Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol. Pharmacol., 64 (4): 994-1005. [PMID:14500756]

6. Santos, WL; Heasley, BH; Jarosz, R; Carter, KM; Lynch, KR; Macdonald, TL. (2004) Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorg. Med. Chem. Lett., 14 (13): 3473-6. [PMID:15177455]

7. 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]

8. Virag, T; Elrod, DB; Liliom, K; Sardar, VM; Parrill, AL; Yokoyama, K; Durgam, G; Deng, W; Miller, DD; Tigyi, G. (2003) Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol. Pharmacol., 63 (5): 1032-42. [PMID:12695531]

9. 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:

Chido Mpamhanga.
Lysophospholipid (LPA) receptors: LPA2 receptor. Last modified on 01/02/2013. Accessed on 25/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=273.


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