General Information of the Protein
Protein ID
PT04124
Protein Name
Proteinase-activated receptor 2
Secondarily
Protein Name
Coagulation factor II receptor-like 1
G-protein coupled receptor 11
Thrombin receptor-like 1
Gene Name
F2RL1
Secondarily
Gene Name
GPR11
PAR2
Sequence
MRSPSAAWLLGAAILLAASLSCSGTIQGTNRSSKGRSLIGKVDGTSHVTGKGVTVETVFSVDEFSASVLTGKLTTVFLPIVYTIVFVVGLPSNGMALWVFLFRTKKKHPAVIYMANLALADLLSVIWFPLKIAYHIHGNNWIYGEALCNVLIGFFYGNMYCSILFMTCLSVQRYWVIVNPMGHSRKKANIAIGISLAIWLLILLVTIPLYVVKQTIFIPALNITTCHDVLPEQLLVGDMFNYFLSLAIGVFLFPAFLTASAYVLMIRMLRSSAMDENSEKKRKRAIKLIVTVLAMYLICFTPSNLLLVVHYFLIKSQGQSHVYALYIVALCLSTLNSCIDPFVYYFVSHDFRDHAKNALLCRSVRTVKQMQVSLTSKKHSRKSSSYSSSSTTVKTSY
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Protease-activated receptor
>
Protease-activated receptor
Function
Receptor for trypsin and trypsin-like enzymes coupled to G proteins (PubMed:28445455). Its function is mediated through the activation of several signaling pathways including phospholipase C (PLC), intracellular calcium, mitogen-activated protein kinase (MAPK), I-kappaB kinase/NF-kappaB and Rho (PubMed:28445455). Can also be transactivated by cleaved F2R/PAR1. Involved in modulation of inflammatory responses and regulation of innate and adaptive immunity, and acts as a sensor for proteolytic enzymes generated during infection. Generally is promoting inflammation. Can signal synergistically with TLR4 and probably TLR2 in inflammatory responses and modulates TLR3 signaling. Has a protective role in establishing the endothelial barrier; the activity involves coagulation factor X. Regulates endothelial cell barrier integrity during neutrophil extravasation, probably following proteolytic cleavage by PRTN3 (PubMed:23202369). Proposed to have a bronchoprotective role in airway epithelium, but also shown to compromise the airway epithelial barrier by interrupting E-cadherin adhesion (PubMed:10086357). Involved in the regulation of vascular tone; activation results in hypotension presumably mediated by vasodilation. Associates with a subset of G proteins alpha subunits such as GNAQ, GNA11, GNA14, GNA12 and GNA13, but probably not with G(o)-alpha, G(i) subunit alpha-1 and G(i) subunit alpha-2. However, according to PubMed:21627585 can signal through G(i) subunit alpha. Believed to be a class B receptor which internalizes as a complex with arrestin and traffic with it to endosomal vesicles, presumably as desensitized receptor, for extended periods of time. Mediates inhibition of TNF-alpha stimulated JNK phosphorylation via coupling to GNAQ and GNA11; the function involves dissociation of RIPK1 and TRADD from TNFR1. Mediates phosphorylation of nuclear factor NF-kappa-B RELA subunit at 'Ser-536'; the function involves IKBKB and is predominantly independent of G proteins. Involved in cellular migration. Involved in cytoskeletal rearrangement and chemotaxis through beta-arrestin-promoted scaffolds; the function is independent of GNAQ and GNA11 and involves promotion of cofilin dephosphorylation and actin filament severing. Induces redistribution of COPS5 from the plasma membrane to the cytosol and activation of the JNK cascade is mediated by COPS5. Involved in the recruitment of leukocytes to the sites of inflammation and is the major PAR receptor capable of modulating eosinophil function such as pro-inflammatory cytokine secretion, superoxide production and degranulation. During inflammation promotes dendritic cell maturation, trafficking to the lymph nodes and subsequent T-cell activation. Involved in antimicrobial response of innate immune cells; activation enhances phagocytosis of Gram-positive and killing of Gram-negative bacteria. Acts synergistically with interferon-gamma in enhancing antiviral responses. Implicated in a number of acute and chronic inflammatory diseases such as of the joints, lungs, brain, gastrointestinal tract, periodontium, skin, and vascular systems, and in autoimmune disorders.
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Uniprot ID
Primary ID:
P55085

Secondarily ID:
Q13317
Q13346
Q53XJ8
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Ensembl ID
ENSG00000164251
HGNC ID
HGNC:3538
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000925 , 16HBE14o-
Compound ID Compound Name Compound Formula
CP0408480
2-[2-[2-[[(4S)-5-amino-4-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-2-[(2-amino-1,3-thiazole-4-carbonyl)amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentyl]amino]ethoxy]ethoxy]ethyl hexadecanoate
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C57H105N13O11S
 2
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
2
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0378691
prop-2-enyl N-[(4S)-5-amino-4-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[[(2S,3S)-2-[[(2S)-2-(furan-2-carbonylamino)-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentyl]carbamate
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C40H67N11O10
 2
1
EC50 = 138 nM
   TI
   LI
   LO
   TS
2
EC50 = 840 nM
   TI
   LI
   LO
   TS
CP0404961
2-amino-N-((4S,7S,13S,16S)-13-sec-butyl-4-carbamoyl-7-(3-guanidinopropyl)-2,18-dimethyl-6,9,12,15-tetraoxo-5,8,11,14-tetraazanonadecan-16-yl)thiazole-4-carboxamide
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C30H53N11O6S
 2
1
EC50 = 142 nM
   TI
   LI
   LO
   TS
2
EC50 = 1770 nM
   TI
   LI
   LO
   TS
CP0378692
6-amino-N-((4S,7S,13S,16S)-13-sec-butyl-4-carbamoyl-7-(3-guanidinopropyl)-2,18-dimethyl-6,9,12,15-tetraoxo-5,8,11,14-tetraazanonadecan-16-yl)nicotinamide
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C32H55N11O6
 2
1
EC50 = 311 nM
   TI
   LI
   LO
   TS
2
EC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0378690
6-amino-N-((4S,7S,13S,16S)-13-sec-butyl-4-carbamoyl-7-(3-guanidinopropyl)-2,18-dimethyl-6,9,12,15-tetraoxo-5,8,11,14-tetraazanonadecan-16-yl)picolinamide
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C32H55N11O6
 1
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0426362
4-amino-N-((4S,7S,13S,16S)-13-sec-butyl-4-carbamoyl-7-(3-guanidinopropyl)-2,18-dimethyl-6,9,12,15-tetraoxo-5,8,11,14-tetraazanonadecan-16-yl)benzamide
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C33H56N10O6
 1
1
EC50 = 6590 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0143555
2-(6-bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]benzimidazole-5-carboxamide
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C30H27BrN4O3
 1
1 IC50 < 2.5 nM
CP0141624
N-[(2S)-3-cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamide
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C32H42N4O4
 1
1 IC50 = 2000 nM
Clinical Information about the Protein
Target 1 ( Proteinase activated receptor 2 (PAR2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Cirrhosis [ICD-11: DB93]
Patented Agent(s) 1 Patented Agent  1
1 Quinazoline derivative 10 Patented
Cirrhosis
Target 2 ( HUMAN proteinase activated receptor 2 (PAR2) )
Target Type Unknown Type Target