protein

PAR2 Peptide

MBS544118

0.25 mg

250 USD

Blocking Peptide

PAR2 Peptide

[PAR2]

[Coagulation factor II receptor like 1; Coagulation factor II thrombin receptor like 1; F2RL1; G protein coupled receptor 11; GPR11; PAR 2; Proteinase activated receptor 2 antibody Thrombin receptor like 1 antibody]

[proteinase-activated receptor 2; Proteinase-activated receptor 2; proteinase-activated receptor 2; coagulation factor II (thrombin) receptor-like 1; Coagulation factor II receptor-like 1; G-protein coupled receptor 11; Thrombin receptor-like 1]

[PAR2]

[F2rl1; F2rl1; Par2; PAR-2; Gpcr11; Gpcr11; Gpr11; Par2; PAR-2]

PAR2_MOUSE

399

This peptide is directed against a cytoplasmic region of PAR2

Antigenic Blocking Peptide

Store at -20 degree C for long term storage.

Dot Blot, ELISA, Immunohistochemistry, Immunoprecipitation, Western Blot.

Dot Blot: 1:15,000-1:20,000. ELISA: 1:15,000-1:20,000. Immunohistochemistry: 1:50-1:100. Immunoprecipitation: 1:200. Western Blot: 1:250

Immunogen: Synthetic peptide taken within amino acid region 300-370 of Mouse PAR2. Expression: Expressed in various lymphoid tissues and activated B- and T-lymphocytes, strongly up-regulated in B-cells infected with Epstein-Barr virus and T-cells infected with herpesvirus 6 or 7.

Molecular Function: G-protein coupled receptor, Receptor, Transducer. Structure: Interacts with TLR4, COPS5 and TMED2. Also interacts with GNAQ, GNA11, GNA12, GNA13, and GNA14. Subcellular Location: Cell membrane; Multi-pass membrane protein

Overview: Proteinase-activated receptor 2 (PAR2) is a G protein-coupled receptor irreversibly activated by extracellular proteases (1). Activated PAR2 couples to multiple heterotrimeric G-protein subtypes including Gaq, Gai, and Ga12/13 and is rapidly desensitized and internalized following phosphorylation and Beta-arrestins binding. Proteolytic cleavage of PAR2 results in the formation of a new amino terminus that acts like a tethered ligand by binding intramolecularly to receptor to trigger transmembrane signaling. Activated PAR2 also signals independently of Gproteins through its interaction with Beta-arrestins, which promotes sustained mitogen-activated protein kinase (MAPK) signaling, actin remodeling, and cell migration. PAR2 is profoundly localized in the vasculature, especially in endothelial cells, and is implicated in the control of vascular tone and homeostasis. Activation of endothelial PAR2 by endogenous serine protease or by PAR2-activating peptide (PAR2-APs, PAR2 agonist) causes vasodilation in vivo or isolated vessels mainly through nitric oxide (NO) and prostacyclin (PGI2) mechanisms (2). PAR2 is also expressed in certain types of metastatic cancers and stimulates tumor cell migration and invasion.Vascular PAR2 expression is up-regulated by inflammatory cytokines such as tumor necrosis factor alpha (TNF-a).Increased TNF-a expression in type 2 diabetic coronary arterioles induces activation of reactive oxygen species(ROS), leading to endothelial dysfunction. PAR2 activation promotes cell proliferation in various cancer cell types induding colon, gastric, cervical and pancreatic cancer cells. PAR2 agonists induce Cox-2 expression in lung cancer cells, MMP 2/9 production in prostate cancer cells and vascular endothelial growth factor secretion in breast cancer cells (3). PAR2 is also associated with renal cell carcinoma progression. PAR2 activation has been linked to cancer progression, especially metastasis and angiogenesis as well as pro-inflammatory and anti-inflammatory properties depending on the system. Proteases that are released during inflammation and injury cleave PAR2 on primary afferent neurons to cause neurogenic inflammation and hyperalgesia. PAR2-induced thermal hyperalgesia depends on sensitization of transient receptor potential vanilloid receptor 1 (TRPV1), which is gated by capsaicin, protons and noxious heat. PAR2-induced thermal hyperalgesia depends on sensitization of TRPV1 (4). The PAR2 selective antibodies were generated against a synthetic peptide taken within amino acid region 300-370 on mouse PAR2 protein. The PAR2 synthetic peptide was covalently modified to achieve desired antigenic properties and was conjugated to a carrier protein before used as immunogen to raise antibodies in rabbits. The PAR2 antibodies are affinity purified over immobilized immunogenic peptide affinity matrix and stabilized with preservatives for long-term storage. Antigenic blocking peptide (P-PAR2) and western blot positive controls (PC-PAR2) are available. Antibodies can be conjugated to fluorophores or secondary enzymes upon request at nominal cost.

171542817

NP_032000.3

NM_007974.4

P55086

44,752 Da

African Trypanosomiasis Pathway (194387); African Trypanosomiasis Pathway (194323); Class A/1 (Rhodopsin-like Receptors) Pathway (1367055); G Alpha (q) Signalling Events Pathway (1367088); GPCR Downstream Signaling Pathway (1367084); GPCR Ligand Binding Pathway (1367054); GPCRs, Class A Rhodopsin-like Pathway (198308); Gastrin-CREB Signalling Pathway Via PKC And MAPK (1367105); Inflammatory Mediator Regulation Of TRP Channels Pathway (948285); Inflammatory Mediator Regulation Of TRP Channels Pathway (948307)

F2RL1: a G-protein coupled receptor for trypsin and trypsin-like enzymes. Acts as a sensor for proteolytic enzymes generated during infection. Modulates pro-inflammatory responses, and innate and adaptive immunity. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. Activates several signaling molecules including phospholipase C (PLC), mitogen-activated protein kinase (MAPK), IKK/NFkB and Rho. Elevates intracellular calcium. Can also be transactivated by cleaved PAR1. 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, may signal through G(i) subunit alpha. Believed to be a class B receptor that 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. 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 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. 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. Belongs to the G-protein coupled receptor 1 family. Protein type: Receptor, GPCR; Membrane protein, integral; Membrane protein, multi-pass; GPCR, family 1. Cellular Component: early endosome; integral to membrane; integral to plasma membrane; membrane; plasma membrane; pseudopodium. Molecular Function: G-protein alpha-subunit binding; G-protein beta-subunit binding; G-protein coupled receptor activity; heterotrimeric G-protein binding; signal transducer activity; thrombin receptor activity. Biological Process: blood coagulation; defense response to virus; elevation of cytosolic calcium ion concentration; G-protein coupled receptor protein signaling pathway; immune system process; inflammatory response; innate immune response; interleukin-1 beta secretion; leukocyte migration; negative regulation of JNK cascade; negative regulation of toll-like receptor 3 signaling pathway; neutrophil activation; positive regulation of actin filament depolymerization; positive regulation of cell migration; positive regulation of chemotaxis; positive regulation of cytokine secretion during immune response; positive regulation of eosinophil degranulation; positive regulation of glomerular filtration; positive regulation of I-kappaB kinase/NF-kappaB cascade; positive regulation of JNK cascade; positive regulation of leukocyte chemotaxis; positive regulation of phagocytosis, engulfment; positive regulation of phosphoinositide 3-kinase cascade; positive regulation of positive chemotaxis; positive regulation of pseudopodium formation; positive regulation of Rho protein signal transduction; positive regulation of superoxide release; positive regulation of toll-like receptor 2 signaling pathway; positive regulation of toll-like receptor 3 signaling pathway; positive regulation of toll-like receptor 4 signaling pathway; positive regulation of transcription from RNA polymerase II promoter; positive regulation of vasodilation; regulation of blood coagulation; regulation of I-kappaB kinase/NF-kappaB cascade; regulation of JNK cascade; signal transduction; T cell activation during immune response

0.25 mg

250 USD