Nomenclature: PAR2

Family: Proteinase-activated receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 397 5q14.1 F2RL1 coagulation factor II (thrombin) receptor-like 1
Mouse 7 399 13 D1 F2rl1 coagulation factor II (thrombin) receptor-like 1
Rat 7 397 2q12 F2rl1 coagulation factor II (thrombin) receptor-like 1
Previous and Unofficial Names
PAR-2
GPR11
proteinase-activated receptor-2
Proteinase-activated receptor-2 G protein-coupled receptor 11
Proteinase-activated receptor-2, G protein-coupled receptor 11
coagulation factor II receptor-like 1
proteinase-activated receptor 2
thrombin receptor-like 1
Protease-activated receptor-2
Gpcr11
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
serine proteases
Agonist proteases (Human)
Trypsin, tryptase, TF/VIIa, Xa
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
2-furoyl-LIGRLO-amide Hs Full agonist 5.4 pKi 2
pKi 5.4 [2]
GB 110 Hs Agonist 6.55 pEC50 1
pEC50 6.55 (EC50 2.8x10-7 M) [1]
Agonist Comments
2-Furoyl-LIGRLO-NH2 activity was measured via calcium mobilisation in HEK 293 cells which constitutively coexpress human PAR1 and PAR2.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GB88 Hs Antagonist 5.7 pIC50 3
pIC50 5.7 (IC50 2x10-6 M) [3]
Expression Datasets

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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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Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0005085 abnormal gallbladder physiology PMID: 17431214 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0002078 abnormal glucose homeostasis PMID: 17992256 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0003627 abnormal leukocyte tethering or rolling PMID: 11086091 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0001970 abnormal pain threshold PMID: 17623652 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd
MGI:101910  MP:0008872 abnormal physiological response to xenobiotic PMID: 12511586  17304351 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae
MGI:101910  MP:0005501 abnormal skin physiology PMID: 16691196  18156206 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6J
MGI:101910  MP:0000230 abnormal systemic arterial blood pressure PMID: 9918574 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd
MGI:101910  MP:0002733 abnormal thermal nociception PMID: 11433347 
F2rl1tm1Bpd|Tg(MMTV-PyVT)634Mul F2rl1tm1Bpd/F2rl1tm1Bpd,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2rl1 Tg(MMTV-PyVT)634Mul
MGI:101910  MGI:2679594  MP:0010144 abnormal tumor vascularization PMID: 18757438 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd
MGI:101910  MP:0008636 decreased circulating interleukin-18 level PMID: 16260585 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
B6.129S4-F2rl1
MGI:101910  MP:0008127 decreased dendritic cell number PMID: 12759239 
F2rl1tm1Mslb F2rl1tm1Mslb/F2rl1tm1Mslb
involves: 129X1/SvJ * C57BL/6
MGI:101910  MP:0002492 decreased IgE level PMID: 12391252 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0001876 decreased inflammatory response PMID: 17623652 
F2rl1tm1Mslb F2rl1tm1Mslb/F2rl1tm1Mslb
involves: 129X1/SvJ * C57BL/6
MGI:101910  MP:0001876 decreased inflammatory response PMID: 12391252 
F2rl1tm1Bpd|Tg(MMTV-PyVT)634Mul F2rl1tm1Bpd/F2rl1tm1Bpd,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2rl1 Tg(MMTV-PyVT)634Mul
MGI:101910  MGI:2679594  MP:0010269 decreased mammary gland tumor incidence PMID: 18757438 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0008874 decreased physiological sensitivity to xenobiotic PMID: 12511586 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008770 decreased survivor rate PMID: 16434493 
F2r/F2rl1tm1.1Cgh F2r/F2rl1tm1.1Cgh/F2r/F2rl1tm1.1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0008770 decreased survivor rate PMID: 20152175 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
B6.129P2-F2rl1
MGI:101910  MP:0008734 decreased susceptibility to endotoxin shock PMID: 14576054 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0003436 decreased susceptibility to induced arthritis PMID: 12511586 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0005166 decreased susceptibility to injury PMID: 17640968 
F2rl1tm1Jkaw F2rl1tm1Jkaw/F2rl1tm1Jkaw
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0005616 decreased susceptibility to type IV hypersensitivity reaction PMID: 11859856 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008762 embryonic lethality PMID: 16434493 
F2rtm1Ajc|F2rl1tm1Cgh|F2rl3tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh,F2rl3tm1Cgh/F2rl3tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MGI:1298207  MP:0008762 embryonic lethality PMID: 16434493 
F2rtm1.1Cgh|F2rl1tm2Cgh|Tg(Tek-F2r)1Cgh F2rtm1.1Cgh/F2rtm1.1Cgh,F2rl1tm2Cgh/F2rl1tm2Cgh,Tg(Tek-F2r)1Cgh/0
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MGI:4438038  MP:0000914 exencephaly PMID: 20152175 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0002743 glomerulonephritis PMID: 17640968 
F2rl1tm1Cgh F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101910  MP:0005292 improved glucose tolerance PMID: 17992256 
F2r+|F2rtm2Cgh|F2rl1+|F2rl1tm2Cgh F2rtm2Cgh/F2r+,F2rl1tm2Cgh/F2rl1+
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0000928 incomplete cephalic closure PMID: 20152175 
F2rl1tm1Bpd|Tg(MMTV-PyVT)634Mul F2rl1tm1Bpd/F2rl1tm1Bpd,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2rl1 Tg(MMTV-PyVT)634Mul
MGI:101910  MGI:2679594  MP:0010383 increased adenoma incidence PMID: 18757438 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0006060 increased cerebral infarction size PMID: 15647743 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0001846 increased inflammatory response PMID: 15458925 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 16434493 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008735 increased susceptibility to endotoxin shock PMID: 16434493 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6
MGI:101910  MP:0004761 increased susceptibility to induced pancreatitis PMID: 15458925 
F2rl1tm1Wrf F2rl1tm1Wrf/F2rl1tm1Wrf
involves: 129P2/OlaHsd
MGI:101910  MP:0001860 liver inflammation PMID: 16260585 
F2rl1tm1Bpd|Tg(MMTV-PyVT)634Mul F2rl1tm1Bpd/F2rl1tm1Bpd,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2rl1 Tg(MMTV-PyVT)634Mul
MGI:101910  MGI:2679594  MP:0001883 mammary adenocarcinoma PMID: 18757438 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6J
MGI:101910  MP:0002081 perinatal lethality PMID: 9918574 
F2rl1tm1Bpd F2rl1tm1Bpd/F2rl1tm1Bpd
involves: 129P2/OlaHsd * C57BL/6J
MGI:101910  MP:0002082 postnatal lethality PMID: 9918574 
Available Assays
DiscoveRx PathHunter® eXpress F2RL1 HEK 293 β-Arrestin GPCR Assay (Cat no. 93-0235E1CP0M)
PathHunter® eXpress F2RL1 U2OS β-Arrestin GPCR Assay (Cat no. 93-0235E3CP0M)
PathHunter® HEK 293 F2RL1 β-Arrestin Cell Line (Cat no. 93-0235C1)
PathHunter® U2OS F2RL1 β-Arrestin Cell Line (Cat no. 93-0235C3)
more info

REFERENCES

1. Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP. (2010) Novel agonists and antagonists for human protease activated receptor 2. J. Med. Chem.53 (20): 7428-40. [PMID:20873792]

2. McGuire JJ, Saifeddine M, Triggle CR, Sun K, Hollenberg MD. (2004) 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J. Pharmacol. Exp. Ther.309 (3): 1124-31. [PMID:14976230]

3. Suen JY, Barry GD, Lohman RJ, Halili MA, Cotterell AJ, Le GT, Fairlie DP. (2012) Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br. J. Pharmacol.165 (5): 1413-23. [PMID:21806599]

To cite this database page, please use the following:

Morley D. Hollenberg, JoAnn Trejo.
Proteinase-activated receptors: PAR2. Last modified on 17/09/2013. Accessed on 16/09/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=348.

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