PAR2 | Proteinase-activated receptors | IUPHAR/BPS Guide to PHARMACOLOGY

PAR2

Target id: 348

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.  » Email us

   GtoImmuPdb view: OFF :     PAR2 has curated GtoImmuPdb data

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 F2R like trypsin receptor 1
Mouse 7 399 13 D1 F2rl1 coagulation factor II (thrombin) receptor-like 1
Rat 7 397 2q12 F2rl1 F2R like trypsin receptor 1
Previous and Unofficial Names
GPR11 | coagulation factor II receptor-like 1 | Protease-activated receptor-2 | coagulation factor II (thrombin) receptor-like 1
Database Links
Specialist databases
GPCRDB par2_human (Hs), par2_mouse (Mm), par2_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in complex with AZ3451 at 3.6 angstrom resolution.
PDB Id:  5NDZ
Ligand:  AZ3451
Resolution:  3.6Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in complex with AZ8838 at 2.8 angstrom resolution
PDB Id:  5NDD
Ligand:  AZ8838
Resolution:  2.8Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in ternary complex with Fab3949 and AZ7188 at 4.0 angstrom resolution
PDB Id:  5NJ6
Ligand:  AZ7188
Resolution:  4.0Å
Species:  Human
References:  8
Natural/Endogenous Ligands
serine proteases
Agonist proteases (Human)
Trypsin, tryptase, TF/VIIa, Xa

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
Ligand Sp. Action Affinity Units Reference
2-furoyl-LIGRLO-amide Hs Full agonist 5.4 pKi 33
pKi 5.4 [33]
AC264613 Hs Agonist 7.5 pEC50 41
pEC50 7.5 (EC50 3.16x10-8 M) [41]
AY77 Hs Agonist 7.5 pEC50 51
pEC50 7.5 (EC50 3.3x10-8 M) [51]
AC-55541 Hs Agonist 6.7 pEC50 41
pEC50 6.7 (EC50 1.99x10-7 M) [41]
GB110 Hs Agonist 6.6 pEC50 4
pEC50 6.6 (EC50 2.8x10-7 M) [4]
AC-98170 Hs Agonist 5.2 pEC50 41
pEC50 5.2 (EC50 6.31x10-6 M) [41]
SLIGKV-NH2 Hs Agonist - - 26
[26]
SLIGRL-NH2 Hs Agonist - - 26
[26]
trans-cinnamoyl-LIGRLO [N-[3H]propionyl]-NH2 Hs Agonist - - 1
[1]
2-furoyl-LIGRL[N[3H]propionyl]-O-NH2 Hs Agonist - - 16
[16]
2-furoyl-LIGRL[N-(Alexa Fluor 594)-O]-NH2 Hs Agonist - - 16
[16]
[3H]2-furoyl-LIGRL-NH2 Hs Agonist - - 19
[19]
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
AZ8838 Hs Antagonist 6.5 pKd 8
pKd 6.5 (Kd 3.44x10-7 M) [8]
Description: Saturation binding of [3H]-AZ8838 antagonist to wild-type PAR2.
AZ8838 Hs Antagonist 5.6 – 5.8 pIC50 8
pIC50 5.8 (IC50 1.5x10-6 M) [8]
Description: Measuring SLIGRL-NH2-induced IP1 formation
pIC50 5.6 (IC50 2.3x10-6 M) [8]
Description: In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.
GB88 Hs Antagonist 5.7 pIC50 44
pIC50 5.7 (IC50 2x10-6 M) [44]
C391 Hs Antagonist 4.8 – 5.9 pIC50 5
pIC50 5.9 (IC50 1.3x10-6 M) [5]
Description: Antagonism of peptidomimetic-induced PAR2 Ca2+ signalling in 16HBE14o- cells.
pIC50 4.8 (IC50 1.43x10-5 M) [5]
Description: Antagonism of 2-at-LIGRL-NH2-induced ERK phosphorylation in 16HBE14o- cells.
AZ7188 Hs Antagonist 5.2 pIC50 8
pIC50 5.2 (IC50 6x10-6 M) [8]
Description: Antagonism of SLIGRL-NH2-induced IP1 formation.
P2pal18s Hs Antagonist - - 42
[42]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AZ3451 Hs Negative 7.9 pKd 8
pKd 7.9 (Kd 1.35x10-8 M) [8]
Description: In a BIACORE assay.
AZ3451 Hs Negative 7.6 – 8.3 pIC50 8
pIC50 8.3 (IC50 5.4x10-9 M) [8]
Description: In a FLIPR calcium accumulation assay, vs. SLIGRL activation.
pIC50 7.6 (IC50 2.3x10-8 M) [8]
Description: Antagonism of SLIGRL-NH2-induced IP1 formation.
Immunopharmacology Comments
PAR2 receptors have been reported to elicit pain and inflammation through a neurogenic mechanism of action, causing release of substance P, activation of NK1 receptors, and sensitization of TRPV1 voltage-gated ion channels. This action can be negated using a selective NK1 receptor antagonist (L732,138) or a TRPV1 receptor antagonist (capsazepine) [14]. PAR2 receptors are expressed in immune cells of both the innate and adaptive immune systems and have been shown to play a role in several peripheral inflammatory conditions. PAR2 activation has been associated with allergic airway inflammation, and allergic sensitisation. Anti-PAR2 antibody or PAR2 inhibiting pepducin alleviate allergen-induced airway hyperresponsiveness and inflammation in mice [28]. PAR2 expression by astrocytes and microglia within the CNS suggests that PAR2 modulation may be a novel approach for developing therapeutics for CNS disorders with an inflammatory association [6]. A study in obese mice suggests that activation of PAR2 is associated with increased adipose expression of inflammatory factors [28].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 12 GO processes
GO:0002286 T cell activation involved in immune response ISS
GO:0002690 positive regulation of leukocyte chemotaxis IDA
GO:0034137 positive regulation of toll-like receptor 2 signaling pathway IMP
GO:0034140 negative regulation of toll-like receptor 3 signaling pathway IMP
GO:0034141 positive regulation of toll-like receptor 3 signaling pathway IMP
GO:0034145 positive regulation of toll-like receptor 4 signaling pathway IDA
GO:0042119 neutrophil activation IDA
GO:0043311 positive regulation of eosinophil degranulation IDA
GO:0050900 leukocyte migration IDA
GO:0060100 positive regulation of phagocytosis, engulfment IDA
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA
GO:0045087 innate immune response IEA
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0060100 positive regulation of phagocytosis, engulfment IDA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0002286 T cell activation involved in immune response ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 8 GO processes
GO:0002690 positive regulation of leukocyte chemotaxis IDA
GO:0002741 positive regulation of cytokine secretion involved in immune response IDA
GO:0034137 positive regulation of toll-like receptor 2 signaling pathway IMP
GO:0034140 negative regulation of toll-like receptor 3 signaling pathway IMP
GO:0034141 positive regulation of toll-like receptor 3 signaling pathway IMP
GO:0034145 positive regulation of toll-like receptor 4 signaling pathway IDA
GO:0043311 positive regulation of eosinophil degranulation IDA
GO:0070963 positive regulation of neutrophil mediated killing of gram-negative bacterium IDA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0097029 mature conventional dendritic cell differentiation IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 10 GO processes
GO:0002741 positive regulation of cytokine secretion involved in immune response IDA
GO:0010804 negative regulation of tumor necrosis factor-mediated signaling pathway IDA
GO:0035926 chemokine (C-C motif) ligand 2 secretion IDA
GO:0050702 interleukin-1 beta secretion IDA
GO:0072608 interleukin-10 secretion IDA
GO:0072643 interferon-gamma secretion ISS
GO:0090195 chemokine secretion IDA
GO:0090198 negative regulation of chemokine secretion IDA
GO:2000484 positive regulation of interleukin-8 secretion IDA
GO:2000778 positive regulation of interleukin-6 secretion IDA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 5 GO processes
GO:0002690 positive regulation of leukocyte chemotaxis IDA
GO:0035926 chemokine (C-C motif) ligand 2 secretion IDA
GO:0050900 leukocyte migration IDA
GO:0090195 chemokine secretion IDA
GO:0090198 negative regulation of chemokine secretion IDA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 7 GO processes
GO:0002286 T cell activation involved in immune response ISS
GO:0034137 positive regulation of toll-like receptor 2 signaling pathway IMP
GO:0034140 negative regulation of toll-like receptor 3 signaling pathway IMP
GO:0034141 positive regulation of toll-like receptor 3 signaling pathway IMP
GO:0034145 positive regulation of toll-like receptor 4 signaling pathway IDA
GO:0042119 neutrophil activation IDA
GO:0043311 positive regulation of eosinophil degranulation IDA
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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Physiological Consequences of Altering Gene Expression
PAR2 knockout mice have slower activated-protein C-induced wound healing.
Species:  Mouse
Tissue:  Keratinocytes
Technique:  Gene knockouts
References: 
Mice overexpressing PAR2 develop pulmonary hypertension after chronic exposure to cigarette smoke. Smoking in transgenic mice results in muscularisation of intrapulomary vessels, right ventricular hypertrophy, imbalances between vasoconstrictors and vasodilators, and enhanced production of growth factors.
Species:  Mouse
Tissue:  Pulmonary
Technique:  Gene over-expression
References:  13
PAR2 knockout mice develop less metastasis and have longer overall survival in a model of B16 melanoma.
Species:  Mouse
Tissue:  Various
Technique:  Gene knockouts
References:  37
PAR2 is required for normal osteoblast and osteoclast differentiation during skeletal growth and repair. PAR2 knockout mice have lower osteoclast surface, osteoblast surface and osteoid volume.
Species:  Mouse
Tissue:  Bone
Technique:  Gene knockouts
References:  15
PAR2 knockout mice are protected against myocarditis after infection with CVB3. PAR2 knockout decreased viral load and virus replication in cardiomyocytes and cardiac fibroblasts, resulting in decreased markers of cardiac infection.
Species:  Mouse
Tissue:  Cardiac
Technique:  Gene knockouts
References:  48
PAR2 deficient mice are protected against allergic sensitisation to common allergens. PAR2 knockout mice did not develop airway inflammation after sensitisation to house dust mite and German cockroach feces.
Species:  Mouse
Tissue:  Various
Technique:  Gene knockouts
References:  11-12,27,38,45
PAR2 knockout mice do not exhibit cancer-related pain behaviours. PAR2 deficient mice show reduced nociceptive pain markers in response to carcinoma-induced pain.
Species:  Mouse
Tissue:  Dorsal root ganglion, bone, head and neck carcinoma.
Technique:  Gene knockouts
References:  24,30
PAR2 deficient mice are protected against rheumatoid arthritis. PAR2 deficient mice have lower arthritis scores, produce less interleukin-17, synovial fibroblasts have slower rates of proliferation and invasion.
Species:  Mouse
Tissue:  Joints, spleen, lymph
Technique:  Gene knockouts
References:  7,10,50
After scrapie (prion) infection, PAR2 knockout mice had delayed onset of clinical symptoms and prolonged survival rates.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knockouts
References:  32
PAR2 knockout mice have reduced hepatic fibrosis. PAR2 deficiency reduced progression of liver fibrosis, hepatic collagen gene expression and hydroxyproline content in response to surgical destabilisation of the medial meniscus.
Species:  Mouse
Tissue:  Liver
Technique:  Gene knockouts
References:  23
PAR2 deficiency limits effects of osteoarthritis on cartilage in mice. PAR2 knockout mice had less knee swelling, less severe lesions and reduced subchondral bone surface.
Species:  Mouse
Tissue:  Cartilage
Technique:  Gene knockouts
References:  2,7
Mice lacking PAR2 are protected from weight gain and insulin resistance induced by a high-fat diet. PAR2 deficiency also confers protection from adipose tissue macrophage inflammation.
Species:  Mouse
Tissue:  Adipose tissue
Technique:  Gene knockouts
References:  3
PAR2 promotes vaccine-induced protection against Helicobacter infection in mice. PAR2 knockout mice have delayed spontaneous breast cancer development.
Species:  Mouse
Tissue:  Breast tissue
Technique:  Gene knockouts
References:  39,47
PAR2 knockout mice are protected against periodontal bone resorption and tissue destruction in models of chronic periodontitis. PAR2 knockout mice have less bone resorption and decreased mast cell infiltration and T-cell activation.
Species:  Mouse
Tissue:  Bone
Technique:  Gene knockouts
References:  49
PAR2 knockout mice are more susceptible to influenza A infection and had more severe associated lung inflammation.
Species:  Mouse
Tissue:  Pulmonary
Technique:  Gene knockouts
References:  22
PAR2 knockout mice have elevated systolic arterial and pulse blood pressures. Gene deletion is associated with moderate elevation of systolic arterial pressure and pulse pressure in response to salt loading and angiotensin II infusion.
Species:  Mouse
Tissue:  Cardiovascular
Technique:  Gene knockouts
References:  34
PAR2 deficient mice have reduced renal inflammation markers in crescentic glomerulonephritis. PAR2 deficient mice had reduced crescent formation, proteinuria, serum creatinine and glomerular fibrin deposition in response to anti-glomerular basement membrane antibody-induced glomerulonephritis.
Species:  Mouse
Tissue:  Renal
Technique:  Gene knockouts
References:  35
PAR2 protects against pancreatitis. PAR2 knockout mice display more severe pancreatitis than wild type mice.
Species:  Mouse
Tissue:  Pancreas
Technique:  Gene knockouts
References:  20,43
PAR2 is required for revascuarisation in a model of hypoxia-induced angiogenesis. Genetic deletion of PAR2 abolished revascularisation of tissue-factor cytoplasmic domain-deleted mice.
Species:  Mouse
Tissue:  Cardiovascular
Technique:  Gene knockouts
References:  46
PAR2 deletion reduces inflammatory markers of Clostridium difficile toxin A enteritis. PAR2 knockout mice had decreased luminal fluid secretion, epithelial damage, edema and neutrophil infiltration.
Species:  Mouse
Tissue:  Epithelium
Technique:  Gene knockouts
References:  9
PAR2 knockout mice have a decreased inflammatory response and reduced alveolar bone loss after infection with Porphyromonas gingivalis.
Species:  Mouse
Tissue:  Oral subcutaneous tissue and bone
Technique:  Gene knockouts
References:  17
PAR2-deficiency reduces levels of neuroinflammatory markers in experimental models of autoimmune encephalomyelitis and multiple sclerosis. PAR2 knockout mice had reduced inflammatory gene expression, demyelination and axonal injury in response to induced autoimmune encephalitis.
Species:  Mouse
Tissue:  CNS
Technique:  Gene knockouts
References:  36
PAR2-deficiency increases acute focal ischemic brain injury. PAR2 knockout mice had increased infarct volume, decreased extraceullar signal-regulated kinase activation and reactive astroglial activation.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knockouts
References:  18
PAR2-deficiency reduces markers of cutaneous inflammation. PAR2 knockout mice had decreased ear-swelling responses, plasma extravasation and leucocyte adherence in models of allergic and toxic dermatitis.
Species:  Mouse
Tissue:  Cutaneous tissue
Technique:  Gene knockouts
References:  21,40
PAR2-deficiency delays onset of microvascular inflammation. PAR2 knockout mice exhibited a decrease in leukocyte rolling flux in microvascular arterioles after surgical trauma.
Species:  Mouse
Tissue:  Vascular, endothelial
Technique:  Gene knockouts
References:  29
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 
Biologically Significant Variants
Type:  Splice variant/deletion
Species:  Human
Description:  6bp-deletion (−133GAGAAG−128) decreased PAR2 mRNA and PXR mRNA expression and led to down regulations of MDR1 and CYP3A4.
References:  31
Type:  Single nucleotide polymorphism
Species:  Human
Description:  Subjects with SNP (c.621C>T) had higher serum IgE and eosinophil count, indicating a higher risk of atopy.
Nucleotide change:  c.621C>T
SNP accession: 
References:  25

References

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1. Al-Ani B, Saifeddine M, Kawabata A, Renaux B, Mokashi S, Hollenberg MD. (1999) Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands. J. Pharmacol. Exp. Ther., 290 (2): 753-60. [PMID:10411588]

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51. Yau MK, Suen JY, Xu W, Lim J, Liu L, Adams MN, He Y, Hooper JD, Reid RC, Fairlie DP. (2016) Potent Small Agonists of Protease Activated Receptor 2. ACS Med Chem Lett, 7 (1): 105-10. [PMID:26819675]

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How to cite this page

Nigel Bunnett, Kathryn DeFea, Justin Hamilton, Morley D. Hollenberg, Rithwik Ramachandran, JoAnn Trejo.
Proteinase-activated receptors: PAR2. Last modified on 02/08/2017. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=348.