Results 21 to 30 of about 313,816 (251)

Biased Signaling by Agonists of Protease Activated Receptor 2 [PDF]

ACS Chemical Biology, 2017
Protease activated receptor 2 (PAR2) is associated with metabolism, obesity, inflammatory, respiratory and gastrointestinal disorders, pain, cancer, and other diseases. The extracellular N-terminus of PAR2 is a common target for multiple proteases, which cleave it at different sites to generate different N-termini that activate different PAR2-mediated ...
Yuhong Jiang, Mei-Kwan Yau, W. Mei Kok, Junxian Lim, Kai-Chen Wu, Ligong Liu, Timothy A. Hill, Jacky Y. Suen, David P. Fairlie   +8 more
openaire   +4 more sources

Electroacupuncture Relieves Visceral Hypersensitivity via Balancing PAR2 and PAR4 in the Descending Pain Modulatory System of Goats

Brain Sciences, 2023
Electroacupuncture (EA) is an efficient treatment for visceral hypersensitivity (VH). However, the mechanism underlying VH remains obscure. This study aimed to examine the effect of EA at Housanli acupoint on PAR2 and PAR4 expression in the ...
Panpan Guo, Qiulin Zhang, Sha Nan, Haolong Wang, Ning Ma, Faisal Ayub Kiani, Mingxing Ding, Jianguo Chen   +7 more
doaj   +1 more source

Activated factor X signaling via protease-activated receptor 2 suppresses pro-inflammatory cytokine production from lipopolysaccharide-stimulated myeloid cells

Haematologica, 2014
Vitamin K-dependent proteases generated in response to vascular injury and infection enable fibrin clot formation, but also trigger distinct immuno-regulatory signaling pathways on myeloid cells.
Eimear M. Gleeson, James S. O’Donnell, Emily Hams, Fionnuala Ní Áinle, Bridget-Ann Kenny, Padraic G. Fallon, Roger J.S. Preston   +6 more
doaj   +1 more source

Antagonism of Protease Activated Receptor-2 by GB88 Reduces Inflammation Triggered by Protease Allergen Tyr-p3

Frontiers in Immunology, 2021
The occurrence of allergic diseases induced by aeroallergens has increased in the past decades. Among inhalant allergens, mites remain the important causal agent of allergic diseases.
Yun-Ju Wang, Sheng-Jie Yu, Jaw-Ji Tsai, Jaw-Ji Tsai, Ching-Hsiang Yu, En-Chih Liao, En-Chih Liao   +6 more
doaj   +1 more source

Protease activated receptor 2 and the cardiovascular system [PDF]

British Journal of Pharmacology, 2002
Protease activated receptors (PARs) represent a novel class of seven transmembrane domain G-protein coupled receptors activated by proteolytic cleavage. Up to now, four members of this class of receptors have been identified, PAR1 to PAR4 (Hollenberg, 1999). The mechanism for activation of PARs involves a proteolytic unmasking of an N-terminal sequence
openaire   +3 more sources

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Communications Biology, 2020
Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other ...
Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker   +17 more
doaj   +1 more source

Protease-Activated Receptor-2 Regulates Neuro-Epidermal Communication in Atopic Dermatitis

Frontiers in Immunology, 2020
Background: Activation of protease-activated receptor-2 (PAR2) has been implicated in inflammation, pruritus, and skin barrier regulation, all characteristics of atopic dermatitis (AD), as well as Netherton syndrome which has similar characteristics ...
Timo Buhl, Timo Buhl, Akihiko Ikoma, Akihiko Ikoma, Cordula Kempkes, Ferda Cevikbas, Mathias Sulk, Mathias Sulk, Joerg Buddenkotte, Joerg Buddenkotte, Tasuku Akiyama, Tasuku Akiyama, Debbie Crumrine, Eric Camerer, Earl Carstens, Michael P. Schön, Peter Elias, Shaun R. Coughlin, Martin Steinhoff, Martin Steinhoff, Martin Steinhoff, Martin Steinhoff, Martin Steinhoff, Martin Steinhoff, Martin Steinhoff   +24 more
doaj   +1 more source

Microparticle-associated endothelial protein C receptor and the induction of cytoprotective and anti-inflammatory effects

Haematologica, 2009
Background The endothelial protein C receptor plays an important role within the protein C pathway in regulating coagulation and inflammation. Recently, we described that endothelial protein C receptor can be released in vitro in microparticulate form ...
Margarita Pérez-Casal, Colin Downey, Beatriz Cutillas-Moreno, Mirko Zuzel, Kenji Fukudome, Cheng Hock Toh   +5 more
doaj   +1 more source

Abrogation of Bronchial Eosinophilic Inflammation and Attenuated Eotaxin Content in Protease-Activated Receptor 2-Deficient Mice

Journal of Pharmacological Sciences, 2005
Protease-activated receptor 2 (PAR2) belongs to the PAR family (PAR1 to PAR4), which is activated by serine proteases (trypsin, tryptase, etc.). In this study, we evaluated the role of PAR2 in allergic inflammation of airways using PAR2-deficient (PAR2−/−
Toshiaki Takizawa, Masaki Tamiya, Takuya Hara, Jiro Matsumoto, Naohiro Saito, Toru Kanke, Junichi Kawagoe, Yukio Hattori   +7 more
doaj   +1 more source

Rheumatic Disease: Protease-Activated Receptor-2 in Synovial Joint Pathobiology

Frontiers in Endocrinology, 2018
Protease-activated receptor-2 (PAR2) is one member of a small family of transmembrane, G-protein-coupled receptors. These receptors are activated via cleavage of their N terminus by serine proteases (e.g., tryptase), unveiling an N terminus tethered ...
Kendal McCulloch, Sarah McGrath, Carmen Huesa, Lynette Dunning, Gary Litherland, Anne Crilly, Leif Hultin, William R. Ferrell, John C. Lockhart, Carl S. Goodyear   +9 more
doaj   +1 more source