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Category Symbol Source: HGNC EntrezGene Ensembl GeneCards RNA genes CroW21

GIFtS
-

F2RL1 Gene

protein-coding GIFtS: 62
GCID: GC05P076120

coagulation factor II (thrombin) receptor-like 1

(Previous symbol: GPR11)

Explore 105 diseases affiliated with
F2RL1 via

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(According to ¹HGNC, ²Entrez Gene,
³UniProtKB/Swiss-Prot, ⁴UniProtKB/TrEMBL, ⁵OMIM, ⁶GeneLoc, ⁷Ensembl, ⁸DME, ⁹miRBase, and/or ¹⁰fRNAdb)
About This Section

Aliases
Coagulation Factor II (Thrombin) Receptor-Like 1¹ ²		G-Protein Coupled Receptor 11² ³
GPR11¹ ² ³ ⁵		Protease-Activated Receptor 2²
PAR2¹ ² ³ ⁵		Proteinase-Activated Receptor 2²
Coagulation Factor II Receptor-Like 1² ³		PAR-2³
Thrombin Receptor-Like 1² ³

External Ids:	HGNC: 3538¹	Entrez Gene: 2150²	Ensembl: ENSG00000164251⁷	OMIM: 600933⁵	UniProtKB: P55085³

Export aliases for F2RL1 gene to outside databases

Previous GC identifers: GC05P074920 GC05P076349 GC05P076153 GC05P076198 GC05P076150 GC05P071322

(According to Entrez Gene, Tocris Bioscience, Wikipedia's Gene Wiki, PharmGKB,
UniProtKB/Swiss-Prot, and/or UniProtKB/TrEMBL)
About This Section

Entrez Gene summary for F2RL1:

Coagulation factor II (thrombin) receptor-like 1 (F2RL1) is a member of the large family of 7-transmembrane-region

receptors that couple to guanosine-nucleotide-binding proteins. F2RL1 is also a member of the protease-activated

receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its

extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. The

F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83%

identical to the mouse receptor sequence. (provided by RefSeq, Jul 2008)

UniProtKB/Swiss-Prot: PAR2_HUMAN, P55085

Function: Receptor for trypsin and trypsin-like enzymes coupled to G proteins. 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. 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. Proposed to have a bronchoprotective role in

airway epithelium, but also shown to compromise the airway epithelial barrier by interrupting E-cadherin adhesion.

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 G alpha-q, G alpha-11, G alpha-14, G alpha-12 and G

alpha-13, 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 G alpha-q/11; 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 G alpha-q/11 and involves promotion of cofilin dephosphoryltaion 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 proinflammatory 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 immnune 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

summary for F2RL1:

Protease-activated receptors (PARs, also known as thrombin receptors) are G-protein-coupled receptors,

activated by cleavage of their N-terminal domains by serine proteases. Hydrolysis reveals a tethered peptide

ligand, which interacts with the receptor within extracellular loop-2 to affect transmembrane signaling.

Four subtypes of receptors have so far been cloned (PAR1-4). PAR2 is expressed in vascular tissue and highly

vascular organs, which indicates a role for this receptor in the regulation of vascular tone. Trypsin is the

endogenous agonist for PAR2 and receptor activation has been coupled to the nitric oxide signaling pathway,

causing vasodilation and hypotension. PAR2 is implicated in chronic responses associated with vessel

inflammation and wound healing. This receptor stimulates activation of T-cells and neutrophils, promotes

leukocyte rolling, adhesion and extravasation, increases capillary permeability and enhances production of

cytokines. In addition to its vascular roles, PAR2 has multiple functions in the gastrointestinal tract. It

is strongly expressed in enterocytes and stimulates prostaglandin (PG) E2 and PGF1alpha synthesis.

Pancreatic PAR2 expression and activation promotes secretory function, in particular increases amylin

secretion.

Gene Wiki entry for F2RL1 (Protease activated receptor 2)

(According to GeneLoc and/or HGNC, and/or
Entrez Gene (NCBI build 37),
and/or miRBase,
Genomic Views according to UCSC (hg19) and Ensembl (release 69), Regulatory elements and Epigenetics data according to QIAGEN, SABiosciences, and/or SwitchGear Genomics)
About This Section

RefSeq DNA sequence:

NC_000005.9 NC_018916.1 NT_006713.15

Regulatory elements:

SABiosciences Regulatory transcription factor binding sites in the F2RL1 gene promoter:
AREB6 c-Fos RFX1 AP-1 HNF-1 Sox9 c-Jun HNF-1A GATA-1
Other transcription factors

SwitchGear Promoter luciferase reporter plasmid: F2RL1 promoter sequence

Search SABiosciences Chromatin IP Primers for F2RL1

Epigenetics:

QIAGEN PyroMark CpG Assay predesigned Pyrosequencing DNA Methylation assays in human, mouse, rat F2RL1

Genomic Location:
Genomic View: UCSC Golden Path with GeneCards custom track

Entrez Gene cytogenetic band: 5q13 Ensembl cytogenetic band: 5q13.3 HGNC cytogenetic band: 5q13

F2RL1 Gene in genomic location: bands according to Ensembl, locations according to (and/or Entrez Gene and/or Ensembl if different)
F2RL1 gene location

GeneLoc information about chromosome 5 GeneLoc Exon Structure

GeneLoc location for GC05P076120: view genomic region (about GC identifiers)

Start:	76,114,758 bp from pter	End:	76,131,140 bp from pter
Size:	16,383 bases	Orientation:	plus strand

(According to ¹UniProtKB, HORDE, neXtProt, Ensembl, and/or Reactome, Modification sites according to ²PhosphoSitePlus, Specific Peptides from DME, Protein expression images according to data from SPIRE MOPED and PaxDb, RefSeq according to NCBI, PDB rendering according to OCA and/or Proteopedia, Recombinant Proteins from EMD Millipore, R&D Systems, GenScript, Enzo Life Sciences, OriGene, Novus Biologicals, Sino Biological, ProSpec, and/or Uscn,
Biochemical Assays by EMD Millipore, R&D Systems, OriGene, GenScript, Cell Signaling Technology, Enzo Life Sciences, and/or Uscn, Ontologies according to Gene Ontology Consortium 01 Mar 2013 and Entrez Gene, Antibodies by EMD Millipore, R&D Systems, GenScript, Cell Signaling Technology, OriGene, Novus Biologicals, Thermo Fisher Scientific, Abcam, and/or Uscn)
About This Section

UniProtKB/Swiss-Prot: PAR2_HUMAN, P55085 (See protein sequence)

Recommended Name: Proteinase-activated receptor 2 precursor

Size: 397 amino acids; 44126 Da

Subunit: Interacts with TLR4, COPS5 and TMED2. Interacts with GNAQ, GNA11, GNA12, GNA13 and GNA14 (By similarity)

Subcellular location: Cell membrane; Multi-pass membrane protein

Miscellaneous: Synthetic PAR agonist peptides (APs) that mimic the first six amino acids of the newly formed N-terminus

activate the native, uncleaved receptor nonenzymatically by binding directly to the corresponding second extracellular

loop to mediate signaling

Secondary accessions: Q13317 Q13346 Q53XJ8

Explore the universe of human proteins at neXtProt for F2RL1: NX_P55085

Post-translational modifications:

A proteolytic cleavage generates a new N-terminus that functions as a tethered ligand. Activating serine proteases

include trypsin, mast cell tryptase, coagulation factors VII and Xa, myeloblastin/PRTN3 and membrane-type serine

protease 1/ST14. Proposed subsequent cleaveage by serine proteases is leading to receptor deactivation and include

neutrophil elastase and cathepsin G. At least in part, implicated proteases are also shown to activate the receptor;

the glycosylation status of the receptor is thought to contribute to the difference. In addition to conventional

trypsin-like proteases is proposed to be activated by other proteases and glycosidases derived from bacteria, fungi

and insects: serine protease allergens such as dust mite Der p3 and Der p9 and mold Pen c13, Porphyromonas gingivalis

arginine-specific (trypsin-like) cysteine proteinases called gingipains, Streptomyces griseus exogenous chitinase, and

an Alternaria alternata aspartate protease. Cleavage by the Alternaria alternata aspartate protease generates

non-conventional processed forms¹

N-glycosylated and sialylated¹

Multiple phosphorylated on serine and threonine residues in the cytoplasmic region upon receptor activation; required

for receptor desensitization and recruitment of beta-arrestin¹

Monoubiquitinated by CBL at the plasma membrane and in early endosomes; not required for receptor endocytosis but for

translocation to late endosomes or lysosomes. Deubiquitination involves STAMBP and USP8; required for lysosomal

trafficking and receptor degradation¹

View modification sites using PhosphoSitePlus²

View neXtProt modification sites for NX_P55085

F2RL1 Protein expression data from MOPED and PaxDb: About this image

REFSEQ proteins: NP_005233.3

ENSEMBL proteins:

ENSP00000425622 ENSP00000296677

Reactome Protein details: P55085
Human Recombinant Protein Products:

	EMD Millipore Purified and/or Recombinant F2RL1 Protein
	Browse R&D Systems for human recombinant proteins
	Browse recombinant and purified proteins available from Enzo Life Sciences
	Browse OriGene full length recombinant human proteins expressed in human HEK293 cells OriGene Protein Over-expression Lysate: F2RL1 OriGene Custom Protein Services for F2RL1
	GenScript Custom Purified and Recombinant Proteins Services for F2RL1
	Novus Biologicals F2RL1 Proteins Novus Biologicals F2RL1 Lysate
	Browse Sino Biological Recombinant Proteins
	Browse ProSpec Recombinant Proteins
	Uscn Proteins for F2RL1

Gene Ontology (GO): 5 cellular component terms (GO ID links to tree view): About this table

GO ID	Qualified GO term	Evidence	PubMed IDs
GO:0005794	Golgi apparatus	TAS	8615752
GO:0005886	plasma membrane	TAS	--
GO:0005887	integral to plasma membrane	IDA	17848177
GO:0016021	integral to membrane	--	--
GO:0031143	pseudopodium	ISS	--

F2RL1 for ontologies About GeneDecksing

F2RL1 Antibody Products:

	EMD Millipore Mono- and Polyclonal Antibodies for the study of F2RL1
	R&D Systems Antibodies for F2RL1 (PAR2)
	Cell Signaling Technology (CST) Antibodies for F2RL1
	Browse OriGene Antibodies OriGene Custom Antibody Services for F2RL1
	GenScript Custom Superior Antibodies Services for F2RL1
	Novus Biologicals F2RL1 Antibodies
	Search for Antibodies for F2RL1 at Abcam
	Uscn Antibodies for F2RL1
	Search ThermoFisher Antibodies for F2RL1

Assay Products for F2RL1:

	Browse Kits and Assays available from EMD Millipore
	OriGene Custom Immunoassay Development Browse OriGene Fluorogenic Cell Assay Kits
	Browse R&D Systems for biochemical assays
	GenScript F2RL1-overexpressing Cell Line for Assay
	Browse Enzo Life Sciences for kits & assays
	Uscn ELISAs and CLIAs for F2RL1

(According to InterPro, ProtoNet, UniProtKB, and/or BLOCKS, Sets of similar genes according to GeneDecks)
About This Section

F2RL1 for domains About GeneDecksing

4 InterPro domains/families:

IPR002281 Pro_rcpt_2

IPR017452 GPCR_Rhodpsn_7TM

IPR003912 Protea_act_rcpt

IPR000276 GPCR_Rhodpsn

Graphical View of Domain Structure for InterPro Entry P55085

ProtoNet protein and cluster: P55085

2 Blocks protein families:

IPB002281 Protease activated receptor 2 precursor signature

IPB003912 Protease activated receptor precursor signature

UniProtKB/Swiss-Prot: PAR2_HUMAN, P55085

Similarity: Belongs to the G-protein coupled receptor 1 family

(According to ¹UniProtKB, Genatlas, LifeMap Discovery™, IUBMB, and/or ²DME, Human phenotypes from GenomeRNAi, Animal models from MGI Mar 06 2013,
bound targets from SABiosciences, miRNA Gene Targets from miRTarBase shRNA from OriGene, RNAi from EMD Millipore, siRNAs from OriGene, QIAGEN, microRNA from QIAGEN, Gene Editing from DNA2.0, Clones from EMD Millipore, OriGene, SwitchGear Genomics, GenScript, Sino Biological, DNA2.0, and Vector BioLabs, Cell Lines from GenScript, LifeMap BioReagents, In Situ Hybridization Assays from Advanced Cell Diagnostics, Ontologies according to Gene Ontology Consortium 01 Mar 2013 via Entrez Gene.)
About This Section

Function Summary: