Results 211 to 220 of about 313,816 (251)

Toward Drugs for Protease-Activated Receptor 2 (PAR2)

Journal of Medicinal Chemistry, 2013
PAR2 has a distinctive functional phenotype among an unusual group of GPCRs called protease activated receptors, which self-activate after cleavage of their N-termini by mainly serine proteases. PAR2 is the most highly expressed PAR on certain immune cells, and it is activated by multiple proteases (but not thrombin) in inflammation.
Yau, Mei-Kwan, Liu, L.igong, Fairlie, David P.   +2 more
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Hepta and octapeptide agonists of protease‐activated receptor 2

Journal of Peptide Science, 2007
AbstractProtease‐activated receptor 2 (PAR2) is a G protein‐coupled cell surface receptor for trypsin‐like enzymes. Proteolytic cleavage at a specific site in the extracellular N‐terminus exposes a receptor‐activating sequence, the ‘tethered ligand’, which binds intramolecularly to initiate receptor signalling.
Devlin, M. G., Pfeiffer, B., Flanagan, B. M., Beyer, R., Cocks, T. M, Fairlie, D. P.   +5 more
openaire   +5 more sources

Expression analysis of protease-activated receptor-2 in cats

Veterinary Immunology and Immunopathology, 2020
Chronic kidney disease (CKD) is a common disease in geriatric cats. Despite its high prevalence, the pathogenesis of feline CKD is poorly understood. Recently, there has been increasing evidence for the role of protease-activated receptor-2 (PAR-2) in the progression of CKD in humans and rodents.
Aki, Iio, Kenjiro, Kaji, Noriyuki, Kaji, Masatoshi, Hori, Tomohiro, Yonezawa, Yasuyuki, Momoi, Shingo, Maeda   +6 more
openaire   +2 more sources

Protease-Activated Receptor-2 Antagonists and Agonists

Current Medicinal Chemistry-Cardiovascular & Hematological Agents, 2003
Interest in the development of specific antagonists of the protease-activated receptors are significant, however, achieving such goals remain extremely challenging. Considerable efforts have been directed at developing specific antagonists of the first elucidated member of this receptor family, namely the thrombin receptor, PAR-1.
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Protease‐activated receptor 2 and gut permeability: a review

Neurogastroenterology & Motility, 2008
Abstract Digestive tract proteases are best known for their proteolytic activity in the digestion of alimentary proteins. However, during the last decade, a possible role of proteases as signalling molecules has been emphasized with the discovery of a novel class of G‐protein coupled receptors located on cell membranes that may be activated by ...
L, Bueno, J, Fioramonti
openaire   +2 more sources

Protease-activated receptor 2: activation, signalling and function

Biochemical Society Transactions, 2003
PARs (protease-activated receptors) are a family of four G-protein-coupled receptors for proteases from the circulation, inflammatory cells and epithelial tissues. This report focuses on PAR2, which plays an important role in inflammation and pain.
G S, Cottrell, S, Amadesi, F, Schmidlin, N, Bunnett   +3 more
openaire   +2 more sources

Expression of Protease-Activated Receptor 2 in Ulcerative Colitis

Inflammatory Bowel Diseases, 2003
Although tryptase released from mast cells might play a key role in the pathogenesis of ulcerative colitis (UC), the role of protease-activated receptor 2 (PAR2), tryptase receptor, remains unclear in the pathogenesis of this disease. The expressions of PAR2 and tumor necrosis factor (TNF) alpha in nine UC tissues and nine normal tissues were examined ...
Jin-A, Kim, Suck-Chei, Choi, Ki-Jung, Yun, Dae-Ki, Kim, Myung-Kwan, Han, Geom-Seog, Seo, Ju-Jin, Yeom, Tae-Hyun, Kim, Yong-Ho, Nah, Young-Mi, Lee   +9 more
openaire   +2 more sources

The protease-activated receptor-2 upregulates keratinocyte phagocytosis

Journal of Cell Science, 2000
ABSTRACT The protease-activated receptor-2 (PAR-2) belongs to the family of seven transmembrane domain receptors, which are activated by the specific enzymatic cleavage of their extracellular amino termini. Synthetic peptides corresponding to the tethered ligand domain (SLIGRL in mouse, SLIGKV in human) can activate PAR-2 without the ...
E R, Sharlow, C S, Paine, L, Babiarz, M, Eisinger, S, Shapiro, M, Seiberg   +5 more
openaire   +2 more sources

Regulating protease activated Receptor 2

2014
Protease-Activated Receptors (PARs) belong to an unusual family of G Protein Coupled Receptors (GPCRs). Each of the four known members is activated by its own N-terminus exposed by proteolytic cleavage and there is no other endogenous agonist known to date.
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A refined agonist pharmacophore for protease activated receptor 2

Bioorganic & Medicinal Chemistry Letters, 2007
Protease activated receptor 2 (PAR(2)) is a G protein-coupled receptor implicated in inflammation and cancer. Only a few peptide agonists are known with greater potency than the native agonist SLIGRL-NH(2). Here we report 52 peptide agonists of PAR(2), 26 with activity at sub-micromolar concentrations, and one being iodinated for radioligand ...
Barry, Grant D., Suen, Jacky Y., Low, Heng Boon, Pfeiffer, Bernhard, Flanagan, Bernadine, Halili, Maria, Le, Giang T., Fairlie, David P.   +7 more
openaire   +5 more sources