Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 14 of 14 for “"PAR2"”.
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Characterisation of novel compounds as antagonists of protease-activated receptor-2 (PAR2)
Protease-activated receptor-2 (PAR2) is a G-protein coupled receptor that is activated through proteolytic cleavage of the N-terminus leading to the coupling to a number of defined second messenger systems though G-protein engagement. Early signalling events such as the mobilisation of …
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Effects of an Endothelial Cell-specific PAR2 Knockout on Endothelium-dependent and -independent Relaxation of Mouse Arteries
Protease-activated receptor 2 (PAR2), a G-protein-coupled receptor expressed on endothelial cells (EC), is a target in chronic inflammatory diseases. Understanding the functions of EC PAR2 will inform the development of PAR2-based therapeutics to treat endothelial dysfunction, a characteristic of …
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Development and Testing of Pharmacological Tools to Evaluate the Role of Protease-Activated Receptor-2 in Allergic Asthma
… central role for Protease-Activated Receptor-2 (PAR2) in allergic asthma pathophysiology have promoted drug development efforts towards this molecular target. I report here that PAR2 antagonist C391 blocks signaling and symptoms caused by the asthma causing allergen Alternaria alternata. I show …
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Characterizing novel protease activated receptor 2 compounds for potential use in examining depression-like behavior
… receptor (GPCR) protease activated receptor 2 (PAR2) has received interest towards its link with depression, as this has shown to play a pro-inflammatory role in disorders of the central nervous system (CNS). However, previously it has remained a challenge to examine PAR2 involvement in …
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Signaling By Protease-Activated Receptors in Gastrointestinal Smooth Muscle
… analysis revealed expression of PARl and PAR2 but not PAR3 or PAR4 in smooth muscle. The PARl agonist TFLLR activated Gq, G12, and Gi3, but not Gil, Gi2, G13, Gs or Gz, whereas the PAR2 agonist SLIGRL activated Gq, G13, Gil, and Gi2, but not Gi3, G12, Gs, or Gz. Both PARl and PAR2 agonists …
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Stress-induced Alterations in Mast Cell Numbers and Proteinase-activated Receptor-2 Expression of the Colon:Role of Corticotrophin-releasing factor
… numbers, and proteinase-activated receptor-2 (PAR2) expression in the rat colon. In addition, we aimed to investigate the involvement of corticotrophin-releasing factor in these stress-related alterations. Eighteen adult rats were divided into 3 experimental groups: (1) a saline-pretreated …
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Mast Cell Influence in the Progression of Post-burn Hypertrophic Scar Pathophysiology
… and activates the protease-activator receptor-2 (PAR2) and activation has proliferative and fibrotic consequences. We demonstrate that PAR2 is highly expressed in post-burn HTSs and, activation sustains fibroproliferative signaling. Co-culture with post-burn HTS fibroblasts and human mast cells …
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G Protein-Coupled Receptor Signaling in Growth and Inflammation of Vascular Smooth Muscle
… are the serine protease-activated receptor PAR2 and the proton sensing receptor GPR68, both identified in vascular smooth muscle cells (VSMCs) and believed to signal through multiple intracellular G proteins. In the stimulatory Gs pathway, activation of cyclic AMP contributes to stimulation …
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The role of intracellular and extracellular cysteines in regulating human proteinase-activated receptor-2 (hPAR2) function
hPAR2, a member of the novel family of proteolytically-activated G-protein coupled receptors termed Proteinase-Activated Receptors (PAR), has recently been implicated in cardiovascular disease. Previous pharmacological studies have found that activation of hPAR2 by mast cell tryptase, (the major …
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Neuroimmune Interactions of Enteric Neurons and Mast Cells: Friends or Foes?
… acting via proteinase activated receptor 2 (PAR2), prostaglandin D2 (PGD2) and interleukin 6 (IL-6). Immunocytochemical examination of rat small and large intestine, revealed frequent co-localization of corticotropin releasing peptide (CRF), known to induce psychological stress reactions in …
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A study of the regulation of oestrogen receptor alpha by tissue factor in breast cancer cells
… ERK1/2 pathway, but was independent of PAR1 and PAR2 activation. Furthermore, exogenous TF suppressed oestradiol-mediated cell proliferation through a pathway partly mediated through PAR2 activation, and also reversed the inhibitory influence of oestradiol on cell invasion. Exogenous TF also …
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Generation and characterization of novel mouse models to validate the role of KLK5 protease in inflammation for pharmacological applications
… promotes skin inflammation via activation of the PAR2-NF-κB-TNFα signaling axis (Briot et al., 2009). In addition, proteolytic cleavage of cathelicidin by KLK5 results in production of antimicrobial and proinflammatory peptides (Yamasaki et al., 2006). Interestingly, the KLK5-PAR2-NF-κB-TNFα …
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The role of C-terminal cysteines in regulating human proteinase-activated receptor-1 function
… have been identified so far in this group—PAR1, PAR2, PAR3 and PAR4. Palmitoylation is the reversible covalent attachment of fatty acids to the cysteine residues of some GPCRs via a thioester linkage; resulting in a fourth intracellular loop. Although recent evidence has suggested that …
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Role of Monocytes and Neutrophils in Thrombosis
… factor or with a protease-activated receptor 2 (PAR2)-specific agonist, even in the complete absence of platelets. Various inhibitors of neutrophil functions and neutrophil granule enzymes were tested to identify the mechanisms involved. Platelets are by far the most well studied cell type …