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  4. Recombinant Human Proteinase-activated receptor 2 (F2RL1)

Recombinant Human Proteinase-activated receptor 2 (F2RL1)

  • 货号：
    CSB-CF007925HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    F2RL1; GPR11; PAR2; Proteinase-activated receptor 2; PAR-2; Coagulation factor II receptor-like 1; G-protein coupled receptor 11; Thrombin receptor-like 1
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full Length of Mature Protein
  • 表达区域：
    37-397aa
  • 氨基酸序列
    SLIGKVDGTSHVTGKGVTVETVFSVDEFSASVLTGKLTTVFLPIVYTIVFVVGLPSNGMALWVFLFRTKKKHPAVIYMANLALADLLSVIWFPLKIAYHIHGNNWIYGEALCNVLIGFFYGNMYCSILFMTCLSVQRYWVIVNPMGHSRKKANIAIGISLAIWLLILLVTIPLYVVKQTIFIPALNITTCHDVLPEQLLVGDMFNYFLSLAIGVFLFPAFLTASAYVLMIRMLRSSAMDENSEKKRKRAIKLIVTVLAMYLICFTPSNLLLVVHYFLIKSQGQSHVYALYIVALCLSTLNSCIDPFVYYFVSHDFRDHAKNALLCRSVRTVKQMQVSLTSKKHSRKSSSYSSSSTTVKTSY
    Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
  • 蛋白标签：
    N-terminal 10xHis-tagged
  • 产品提供形式：
    Liquid or Lyophilized powder
    Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
  • 缓冲液：
    Lyophilized from Tris/PBS-based buffer, 6% Trehalose, pH 8.0
  • 储存条件：
    Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
  • 保质期：
    The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
    Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
  • 货期：
    Basically, we can dispatch the products out in 1-3 working days after receiving your orders. Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
    Note: All of our proteins are default shipped with normal blue ice packs, if you request to ship with dry ice, please communicate with us in advance and extra fees will be charged.
  • 注意事项：
    Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
  • Datasheet & COA：
    Please contact us to get it.

产品评价

靶点详情

  • 功能：
    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. Regulates endothelial cell barrier integrity during neutrophil extravasation, probably following proteolytic cleavage by PRTN3. 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 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 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 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.
  • 基因功能参考文献：
    1. Study findings point out that PAR2 could play an essential role in gastroesophageal reflux disease (GERD) pathogenesis - even repeated short-term exposure to weakly acidic conditions lead to the upregulation of PAR2 and subsequent activation of the intense IL-8 release in the esophageal mucosa and initiation of mucosal immune response in GERD. PMID: 29672302
    2. PAR-2 is expressed basolaterally in airway cells, where it stimulates both intracellular Ca(2+) release and Ca(2+) influx, which activates low-level nitric oxide production, increases apical membrane Cl(-) permeability approximately 3-5-fold, and increases ciliary beating approximately 20-50%. PMID: 28874459
    3. PAR2 signaling from endosomes underlies the persistent hyperexcitability of nociceptors that mediates chronic pain of irritable bowel syndrome. PMID: 30012612
    4. PAR2 plays an important role in the proliferation and metastasis of hepatocellular carcinoma. PMID: 29563756
    5. PAR2 expression is crucial for TGF-beta1-induced ERK activation and cell motility. Functional cooperation of PAR2 and TGF-beta1 involves a physical interaction between PAR2 and ALK5. PMID: 29261154
    6. Activation of PAR2 inhibits the expression of IL-10 in B cells, which can be reversed by treating B cells with Bcl2L12 shRNA-carrying liposomes. PMID: 28426164
    7. High Expressions of PAR2 is associated with cancer. PMID: 28418856
    8. activation of PAR2 compromises the vascular endothelial barrier function by suppressing the expression of Ve-cadherin. PMID: 28485540
    9. plays a direct role in melanogenesis by increasing stem cell factor secretion from keratinocytes PMID: 26909822
    10. Neutrophil elastase enhances IL-12p40 production by lipopolysaccharide-stimulated macrophages via transactivation of the PAR-2/EGFR/TLR4 signaling pathway PMID: 27282560
    11. PAR2 is crucial for TGF-beta1-induced cell motility by its ability to sustain expression of ALK5. Therapeutically targeting PAR2 may thus be a promising approach in preventing TGF-beta-dependent driven metastatic dissemination in PDAC and possibly other stroma-rich tumour types. PMID: 27248167
    12. Protease-activated receptor 2 (PAR2) is present in human skin. PMID: 27981668
    13. PAR2 signaling promotes cancer cell migration through miR-205/BMPR1B pathway in human colorectal carcinoma. PMID: 28990808
    14. findings showed in intestinal epithelial cells that PAR-2 activation leads to polarized IL-8 secretion in accordance with the side of PAR-2 activation, apical or basolateral, but do not affect ubiquitin proteasome system; demonstrate that PAR-2 activation leads to an increased IL-8 production and can affect proteasome system, particularly when PAR-2 activation was induced in the apical side PMID: 27455449
    15. TF-induced microvessel stabilization is regulated via PAR2-SMAD3 that is indispensable for the maintenance of vascular integrity. PMID: 26658897
    16. PAR-2- and PAR-1-mediated TNF-alpha release from monocytes suggests that these unique protease receptors are involved in the pathogenesis of inflammation. PMID: 27423452
    17. Results indicate that chymotrypsin-like serine protease enhances soluble fms-like tyrosine kinase 1 production through protease-activated receptor-2 in trophoblast cells and thus plays an important additional role in preeclampsia pathogenesis. PMID: 27140908
    18. crystal structures of PAR2 in complex with two distinct antagonists and a blocking antibody PMID: 28445455
    19. PAR-2 plays an important role in the progression of ovarian clear cell carcinoma. PMID: 28438620
    20. Data suggest activation of PAR2 via FVIIA/TF signaling activates PI3K/AKT signaling, inactivates GSK3b signaling, leads to accumulation of beta-catenin, and promotes tumor cell migration/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
    21. PAR2 modulation was sufficient to induce islet cell transdifferentiation in the absence of beta-cells. PMID: 27809303
    22. Studies provide increasing evidence that PAR2 plays a significant role in inflammatory diseases both in the periphery and in the 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
    23. 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
    24. Increase in airway smooth muscle mass, possibly involving aberrant expression and activation of PAR-2-mediated pathways, characterizes younger patients with severe asthma with poor asthma control PMID: 27001157
    25. PAR2/GSK3beta is a novel pathway that plays a critical role in the regulation of stem/progenitor cell survival and proliferation in normal colon crypts and colon cancer. PMID: 27313176
    26. Study suggests that deregulated pericellular matriptase activity in OSCC may transactivate PAR-2 on fibroblasts in the surrounding tissue and thus promote their recruitment to the perimeter of the tumor, contributing to a microenvironement that favors tumor growth of oral squamous cell carcinoma. PMID: 27615543
    27. Study demonstrates that AHRR and F2RL3 methylation are strong predictors individually for lung cancer development. PMID: 27924164
    28. PAR2 activation promoted obesity. PMID: 27006943
    29. involved in pathway induced by house dust mites, which has anti-apoptotic effects on neutrophils of normal and allergic subjects PMID: 26666432
    30. Activation of PAR-2 by SLIGRL, a PAR-2 specific ligand, leads to dual phosphorylation of both catalytic sites but primarily regulated eNOS-Thr-495 phosphorylation with no change in nitric oxide production. PMID: 26729042
    31. 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
    32. 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
    33. 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
    34. 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
    35. Binding of the PH domain of PAR-2 enables breast cancer growth and extravillous trophoblast invasion. PMID: 26600192
    36. Results show that exposure of bronchial epithelial cells to Aspergillus fumigatus extract suppressed poly I:C and HRV16 signaling via a mechanism shown to involve activation of PAR-2 and PTPN11. PMID: 26072921
    37. alpha-Enolase increases after injury and may activate pulmonary endothelial cells and prime PMNs through plasmin activity and PAR-2 activation PMID: 25944790
    38. Study showed that PAR-2, in CSF, was not specifically altered in prion diseases compared to other neurodegenerative conditions. PMID: 25886404
    39. HAI-1 may have a critical role in maintaining normal keratinocyte morphology through regulation of PAR-2-dependent p38 mitogen-activated protein kinase signaling. PMID: 25842366
    40. In colorectal cancer, miR-125b mediates PAR2-induced cancer cell migration by targeting Gab2. PMID: 26354435
    41. PAR-2-mediated IL-13 production by human monocytes may be dependent on the Ca2+/ERK2 signaling pathway. PMID: 25976462
    42. Coculture of human cancer cells with murine trigeminal neurons demonstrated colocalization of TMPRSS2 with PAR2. PMID: 25734995
    43. These findings suggested 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
    44. GM-CSF primes IL-13 production by macrophages via PAR-2. PMID: 25633855
    45. Data indicate that PAR2 stimulation induces the production of many key inflammatory mediators. PMID: 26238490
    46. PAR2 up regulated in sebaceous lipogenesis, inflammation and innate immunity. PMID: 25880702
    47. 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
    48. Cytokine induction by diesel exhaust particles is suppressed by PAR-2 silencing in bronchial epithelial cells. PMID: 26160521
    49. PAR-2 regulates the growth and invasion of oral squamous carcinoma cells. PMID: 25912757
    50. PAR2 and TRPV4 are activated by neutrophil elastase to cause inflammation and pain PMID: 25878251

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  • 亚细胞定位：
    Cell membrane; Multi-pass membrane protein.
  • 蛋白家族：
    G-protein coupled receptor 1 family
  • 组织特异性：
    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.
  • 数据库链接：

    HGNC: 3538

    OMIM: 600933

    KEGG: hsa:2150

    STRING: 9606.ENSP00000296677

    UniGene: Hs.744181