F2RL1 Antibody
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Description
Definition and Biological Context
F2RL1 Antibodies are immunoreagents designed to detect or inhibit PAR2, a transmembrane receptor activated by proteolytic cleavage. PAR2 plays roles in vascular regulation, antimicrobial responses, and tumor microenvironment modulation . These antibodies enable researchers to study PAR2's spatial expression, signaling pathways, and interactions with immune checkpoints like PD-1 and CTLA-4 .
Mechanism of Action
F2RL1 antibodies typically function by:
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Blocking ligand binding: Preventing activation by proteases (e.g., trypsin, thrombin) or tethered ligands .
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Inhibiting downstream signaling: Disrupting PLC, MAPK, and NF-κB pathways linked to tumor growth and inflammation .
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Facilitating immune cell infiltration: Counteracting PAR2-mediated suppression of cytotoxic T cells and dendritic cells .
Research Applications
F2RL1 antibodies are utilized in:
Diagnostic Performance in Cervical Cancer
F2RL1 expression distinguishes cervical cancer subtypes and stages:
| Parameter | Squamous Carcinoma | Adenocarcinoma | Normal Tissue |
|---|---|---|---|
| mRNA expression (ΔCt) | 8.2 ± 1.5 | 5.1 ± 0.9 | 1.0 ± 0.3 |
| Protein concentration (ng/mL) | 12.4 ± 2.1 | 7.8 ± 1.4 | 1.2 ± 0.2 |
F2RL1 levels in cervical scrapings show 92% sensitivity for high-grade squamous intraepithelial lesions (HSIL) .
Survival and Immune Correlations
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Prognosis: High F2RL1 expression reduces 5-year survival rates in cervical cancer (OS: 54% vs. 82%; PFS: 48% vs. 75%) .
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Immune evasion: Inverse correlations with immune cell infiltration (e.g., cytotoxic cells: R = -0.31; Tregs: R = -0.28) .
Challenges and Future Directions
Product Specs
Buffer
PBS with 0.1% Sodium Azide, 50% Glycerol, pH 7.3. Store at -20°C. Avoid freeze/thaw cycles.
Lead Time
Typically, we can ship your orders within 1-3 business days after receiving them. Delivery times may vary depending on the purchasing method or location. Please consult your local distributors for specific delivery timeframes.
Synonyms
F2RL1; GPR11; PAR2; Proteinase-activated receptor 2; PAR-2; Coagulation factor II receptor-like 1; G-protein coupled receptor 11; Thrombin receptor-like 1
Target Names
Uniprot No.
Target Background
Function
F2RL1 (Protease-activated receptor 2, PAR2) is a G protein-coupled receptor that binds trypsin and trypsin-like enzymes. Its activation triggers various signaling pathways, including phospholipase C (PLC), intracellular calcium, mitogen-activated protein kinase (MAPK), I-kappaB kinase/NF-kappaB, and Rho. It can also be activated by cleaved F2R/PAR1. PAR2 plays a crucial role in modulating inflammatory responses and regulating both innate and adaptive immunity. It acts as a sensor for proteolytic enzymes produced during infection, generally promoting inflammation. It can synergize with TLR4 and likely TLR2 in inflammatory responses, and modulates TLR3 signaling. PAR2 has a protective role in maintaining the endothelial barrier, which involves coagulation factor X. It regulates endothelial cell barrier integrity during neutrophil extravasation, likely following proteolytic cleavage by PRTN3. PAR2 has been proposed to have a bronchoprotective role in airway epithelium, but has also been shown to compromise the airway epithelial barrier by interrupting E-cadherin adhesion. PAR2 is involved in regulating vascular tone; activation results in hypotension, likely mediated by vasodilation. PAR2 associates with a subset of G protein alpha subunits, including GNAQ, GNA11, GNA14, GNA12, and GNA13, but not with G(o) alpha, G(i) subunit alpha-1, and G(i) subunit alpha-2. However, according to PubMed:21627585, it can signal through G(i) subunit alpha. PAR2 is believed to be a class B receptor that internalizes as a complex with arrestin and traffics with it to endosomal vesicles, presumably as a desensitized receptor, for extended periods of time. PAR2 mediates inhibition of TNF-alpha-stimulated JNK phosphorylation via coupling to GNAQ and GNA11; this function involves dissociation of RIPK1 and TRADD from TNFR1. PAR2 mediates phosphorylation of nuclear factor NF-kappa-B RELA subunit at 'Ser-536'; this function involves IKBKB and is predominantly independent of G proteins. PAR2 is involved in cellular migration, cytoskeletal rearrangement, and chemotaxis through beta-arrestin-promoted scaffolds, independent of GNAQ and GNA11. This function involves promotion of cofilin dephosphorylation and actin filament severing. PAR2 induces redistribution of COPS5 from the plasma membrane to the cytosol, and activation of the JNK cascade is mediated by COPS5. PAR2 participates in the recruitment of leukocytes to sites of inflammation and is the primary PAR receptor capable of modulating eosinophil function, including proinflammatory cytokine secretion, superoxide production, and degranulation. During inflammation, it promotes dendritic cell maturation, trafficking to the lymph nodes, and subsequent T-cell activation. PAR2 plays a role in the antimicrobial response of innate immune cells; activation enhances phagocytosis of Gram-positive bacteria and killing of Gram-negative bacteria. It synergizes with interferon-gamma to enhance antiviral responses. PAR2 has been implicated in a number of acute and chronic inflammatory diseases, such as those affecting the joints, lungs, brain, gastrointestinal tract, periodontium, skin, and vascular systems, as well as autoimmune disorders.
Gene References Into Functions
- Research suggests that PAR2 may play a significant role in the pathogenesis of gastroesophageal reflux disease (GERD), as even repeated short-term exposure to weakly acidic conditions leads to PAR2 upregulation and subsequent IL-8 release in the esophageal mucosa, initiating a mucosal immune response. PMID: 29672302
- PAR-2 is expressed basolaterally in airway cells, where it stimulates both intracellular Ca(2+) release and Ca(2+) influx, activating low-level nitric oxide production, increasing apical membrane Cl(-) permeability by approximately 3-5-fold, and enhancing ciliary beating by approximately 20-50%. PMID: 28874459
- PAR2 signaling from endosomes contributes to the persistent hyperexcitability of nociceptors, which mediates chronic pain associated with irritable bowel syndrome. PMID: 30012612
- PAR2 plays a critical role in the proliferation and metastasis of hepatocellular carcinoma. PMID: 29563756
- PAR2 expression is crucial for TGF-beta1-induced ERK activation and cell motility. Functional cooperation between PAR2 and TGF-beta1 involves a physical interaction between PAR2 and ALK5. PMID: 29261154
- Activation of PAR2 inhibits IL-10 expression in B cells, which can be reversed by treating B cells with Bcl2L12 shRNA-carrying liposomes. PMID: 28426164
- High PAR2 expression is associated with cancer. PMID: 28418856
- Activation of PAR2 compromises vascular endothelial barrier function by suppressing Ve-cadherin expression. PMID: 28485540
- PAR2 plays a direct role in melanogenesis by increasing stem cell factor secretion from keratinocytes. PMID: 26909822
- Neutrophil elastase enhances IL-12p40 production by lipopolysaccharide-stimulated macrophages via transactivation of the PAR-2/EGFR/TLR4 signaling pathway. PMID: 27282560
- PAR2 is crucial for TGF-beta1-induced cell motility due to its ability to sustain ALK5 expression. Targeting PAR2 may therefore be a promising therapeutic approach for preventing TGF-beta-dependent metastatic dissemination in PDAC and potentially other stroma-rich tumor types. PMID: 27248167
- Protease-activated receptor 2 (PAR2) is present in human skin. PMID: 27981668
- PAR2 signaling promotes cancer cell migration through the miR-205/BMPR1B pathway in human colorectal carcinoma. PMID: 28990808
- Studies in intestinal epithelial cells show that PAR-2 activation leads to polarized IL-8 secretion depending on the side of PAR-2 activation (apical or basolateral) but does not affect the ubiquitin proteasome system. However, these studies demonstrate that PAR-2 activation increases IL-8 production and can affect the proteasome system, particularly when PAR-2 activation occurs on the apical side. PMID: 27455449
- TF-induced microvessel stabilization is regulated via PAR2-SMAD3, which is essential for maintaining vascular integrity. PMID: 26658897
- PAR-2- and PAR-1-mediated TNF-alpha release from monocytes suggests that these unique protease receptors play a role in inflammation pathogenesis. PMID: 27423452
- Results indicate that chymotrypsin-like serine protease enhances soluble fms-like tyrosine kinase 1 production through protease-activated receptor-2 in trophoblast cells, playing an additional role in preeclampsia pathogenesis. PMID: 27140908
- Crystal structures of PAR2 in complex with two distinct antagonists and a blocking antibody have been determined. PMID: 28445455
- PAR-2 plays a significant role in the progression of ovarian clear cell carcinoma. PMID: 28438620
- Data suggest that activation of PAR2 via FVIIA/TF signaling activates PI3K/AKT signaling, inactivates GSK3b signaling, leads to beta-catenin accumulation, and promotes tumor cell migration and invasion. (PAR2 = protease-activated receptor 2; FVIIA = coagulation factor VIIa; TF = tissue factor/thromboplastin; PI3K = phosphatidylinositol 3-kinase; AKT = proto-oncogene protein c-akt; GSK3b = glycogen synthase kinase 3 beta) PMID: 28522609
- PAR2 modulation was sufficient to induce islet cell transdifferentiation in the absence of beta-cells. PMID: 27809303
- Studies provide increasing evidence that PAR2 plays a significant role in inflammatory diseases both in the periphery and in the central nervous system (CNS). There is a clear similarity between PAR2 expression and activation on cells of the immune system and those cell types that are proposed to play a role within the CNS, astrocytes, and microglia. [review] PMID: 26648078
- Results show that PAR2 in hepatic stellate cells plays a crucial role in promoting hepatocellular carcinoma growth, presumably by mediating migration and secretion of pro-angiogenic and pro-mitotic factors. PMID: 27473374
- Increased airway smooth muscle mass, possibly involving aberrant PAR-2-mediated pathway expression and activation, characterizes younger patients with severe asthma and poor asthma control. PMID: 27001157
- PAR2/GSK3beta is a novel pathway that plays a critical role in regulating stem/progenitor cell survival and proliferation in normal colon crypts and colon cancer. PMID: 27313176
- Studies demonstrate that deregulated pericellular matriptase activity in OSCC may transactivate PAR-2 on fibroblasts in the surrounding tissue, promoting their recruitment to the tumor perimeter and contributing to a microenvironment that favors tumor growth of oral squamous cell carcinoma. PMID: 27615543
- Studies demonstrate that AHRR and F2RL3 methylation are strong predictors individually for lung cancer development. PMID: 27924164
- PAR2 activation has been linked to obesity. PMID: 27006943
- PAR2 is involved in a pathway induced by house dust mites, which has anti-apoptotic effects on neutrophils in both normal and allergic subjects. PMID: 26666432
- Activation of PAR-2 by SLIGRL, a PAR-2 specific ligand, leads to dual phosphorylation of both catalytic sites but primarily regulates eNOS-Thr-495 phosphorylation with no change in nitric oxide production. PMID: 26729042
- Stimulation of PAR-2 activates Nf-kappaB signaling, resulting in RelA nuclear translocation and enhanced expression of pro-inflammatory mRNAs in oral squamous cell carcinoma. PMID: 26839311
- This study provides evidence for the major role of PAR-2 in the pathogenesis of gastroesophageal reflux disease (GERD) and GERD-associated mucosal alterations. PMID: 25265427
- PAR-2 expression is increased on CD14++CD16+ monocytes in the peripheral blood of subjects with severe asthma, and may be a biomarker of asthma severity. PMID: 26658828
- PAR-2 contributes to the progression of pulmonary fibrosis, and targeting PAR-2 may be a promising therapeutic strategy for treating pulmonary fibrosis. PMID: 26147947
- Binding of the PH domain of PAR-2 enables breast cancer growth and extravillous trophoblast invasion. PMID: 26600192
- Results show that exposure of bronchial epithelial cells to Aspergillus fumigatus extract suppressed poly I:C and HRV16 signaling via a mechanism involving activation of PAR-2 and PTPN11. PMID: 26072921
- Alpha-Enolase increases after injury and may activate pulmonary endothelial cells and prime PMNs through plasmin activity and PAR-2 activation. PMID: 25944790
- Studies showed that PAR-2 in cerebrospinal fluid (CSF) was not specifically altered in prion diseases compared to other neurodegenerative conditions. PMID: 25886404
- HAI-1 may play a critical role in maintaining normal keratinocyte morphology through regulation of PAR-2-dependent p38 mitogen-activated protein kinase signaling. PMID: 25842366
- In colorectal cancer, miR-125b mediates PAR2-induced cancer cell migration by targeting Gab2. PMID: 26354435
- PAR-2-mediated IL-13 production by human monocytes may be dependent on the Ca2+/ERK2 signaling pathway. PMID: 25976462
- Coculture of human cancer cells with murine trigeminal neurons demonstrated colocalization of TMPRSS2 with PAR2. PMID: 25734995
- These findings suggest that the pathophysiology of heartburn sensation or esophageal hypersensitivity may be associated with the activation of PAR-2, TRPV1, and acid-sensing ion channels. PMID: 26294672
- GM-CSF primes IL-13 production by macrophages via PAR-2. PMID: 25633855
- Data indicate that PAR2 stimulation induces the production of many key inflammatory mediators. PMID: 26238490
- PAR2 is upregulated in sebaceous lipogenesis, inflammation, and innate immunity. PMID: 25880702
- Serine protease activity of Per a 10 activates A549 cells to secrete proinflammatory cytokines by PAR-2 activation and Ca(2+) mobilization, and can be exploited therapeutically. PMID: 25468564
- Cytokine induction by diesel exhaust particles is suppressed by PAR-2 silencing in bronchial epithelial cells. PMID: 26160521
- PAR-2 regulates the growth and invasion of oral squamous carcinoma cells. PMID: 25912757
- PAR2 and TRPV4 are activated by neutrophil elastase to cause inflammation and pain. PMID: 25878251
Database Links
Protein Families
G-protein coupled receptor 1 family
Subcellular Location
Cell membrane; Multi-pass membrane protein.
Tissue Specificity
Widely expressed in tissues with especially high levels in pancreas, liver, kidney, small intestine, and colon. Moderate expression is detected in many organs, but none in brain or skeletal muscle. Expressed in endothelial cells.
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