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Protease activated receptor 2

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https://www.readbyqxmd.com/read/29778747/novel-peptide-inhibits-inflammation-by-suppressing-of-protease-activated-receptor-2
#1
Bora Kim, Hyun-Soo Kim
We synthesized and investigated the effects of a novel peptide B, RRFSLLRY as a novel PAR-2 antagonist. Peptide B decreased calcium levels in HaCat cells stimulated with trypsin and PAR-2 activator (SLIGKV) and cytokeratin 14 and PCNA was decreased by peptide B. Peptides B also reduced the expression of inflammatory cytokines such as TNF-α and interleukin-6. Significant increase of oxazolone-induced transepidermal water loss (TEWL) was decreased by the addition of peptide B in hairless mice. These findings suggest that the anti-inflammatory effect of peptide B is due to inhibition of PAR-2 signaling...
May 17, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29772491/calpain-inhibition-reduces-nmda-receptor-rundown-in-rat-substantia-nigra-dopamine-neurons
#2
Jerry Zhao, Michel Baudry, Susan Jones
Repeated activation of N-Methyl-d-aspartate receptors (NMDARs) causes a Ca2+ -dependent reduction in NMDAR-mediated current in dopamine (DA) neurons of the substantia nigra pars compacta (SNc) in one week old rats; however, a Ca2+ -dependent regulatory protein has not been identified. The role of the Ca2+ -dependent cysteine protease, calpain, in mediating NMDAR current rundown was investigated. In brain slices from rats aged postnatal day 7-9 ('P7'), bath application of either of the membrane permeable calpain inhibitors, N-Acetyl-L-leucyl-L-leucyl-L-norleucinal (ALLN, 20 μM) or MDL-28170 (30 μM) significantly reduced whole-cell NMDAR current rundown...
May 4, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29769546/effects-of-the-th2-dominant-milieu-on-allergic-responses-in-der-f-1-activated-mouse-basophils-and-mast-cells
#3
Myung-Hee Yi, Hyoung-Pyo Kim, Kyoung Yong Jeong, Ju Yeong Kim, In-Yong Lee, Tai-Soon Yong
Although basophils and mast cells share similar phenotypic and functional properties, little is known about the difference in the initial Th2 immune responses of these cells following exposure to proteolytic allergens. Here, we investigated the mechanisms of Th2-mediated immune responses in mouse bone marrow-derived basophils (BMBs) and mast cells (BMMCs) via stimulation with the cysteine protease allergen Der f 1. Our results showed that Th2 cytokines were induced from BMBs by active recombinant Der f 1 (rDer f 1 independently with Toll-like receptor (TLR) 2 and TLR4...
May 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29751765/lipophilic-components-of-diesel-exhaust-particles-induce-pro-inflammatory-responses-in-human-endothelial-cells-through-ahr-dependent-pathway-s
#4
Bendik C Brinchmann, Tonje Skuland, Mia H Rambøl, Krisztina Szoke, Jan E Brinchmann, Arno C Gutleb, Elisa Moschini, Alena Kubátová, Klara Kukowski, Eric Le Ferrec, Dominique Lagadic-Gossmann, Per E Schwarze, Marit Låg, Magne Refsnes, Johan Øvrevik, Jørn A Holme
BACKGROUND: Exposure to traffic-derived particulate matter (PM), such as diesel exhaust particles (DEP), is a leading environmental cause of cardiovascular disease (CVD), and may contribute to endothelial dysfunction and development of atherosclerosis. It is still debated how DEP and other inhaled PM can contribute to CVD. However, organic chemicals (OC) adhered to the particle surface, are considered central to many of the biological effects. In the present study, we have explored the ability of OC from DEP to reach the endothelium and trigger pro-inflammatory reactions, a central step on the path to atherosclerosis...
May 11, 2018: Particle and Fibre Toxicology
https://www.readbyqxmd.com/read/29743547/the-protease-activated-receptor2-promotes-rab5a-mediated-generation-of-pro-metastatic-microvesicles
#5
Kaushik Das, Ramesh Prasad, Sreetama Roy, Ashis Mukherjee, Prosenjit Sen
Metastasis, the hallmark of cancer propagation is attributed by the modification of phenotypic/functional behavior of cells to break attachment and migrate to distant body parts. Cancer cell-secreted microvesicles (MVs) contribute immensely in disease propagation. These nano-vesicles, generated from plasma membrane outward budding are taken up by nearby healthy cells thereby inducing phenotypic alterations in those recipient cells. Protease activated receptor 2 (PAR2), activated by trypsin, also contributes to cancer progression by increasing metastasis, angiogenesis etc...
May 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29739329/thrombin-and-factor-xa-link-the-coagulation-system-with-liver-fibrosis
#6
Ameet Dhar, Fouzia Sadiq, Quentin M Anstee, Adam P Levene, Robert D Goldin, Mark R Thursz
BACKGROUND: Thrombin activates hepatic stellate cells via protease-activated receptor-1. The role of Factor Xa (FXa) in hepatic fibrosis has not been elucidated. We aimed to evaluate the impact of FXa and thrombin in vitro on stellate cells and their respective inhibition in vivo using a rodent model of hepatic fibrosis. METHODS: HSC-LX2 cells were incubated with FXa and/or thrombin in cell culture, stained for αSMA and relative gene expression and gel contraction calculated...
May 8, 2018: BMC Gastroenterology
https://www.readbyqxmd.com/read/29728559/chemically-triggered-drug-release-from-an-antibody-drug-conjugate-leads-to-potent-antitumour-activity-in-mice
#7
Raffaella Rossin, Ron M Versteegen, Jeremy Wu, Alisher Khasanov, Hans J Wessels, Erik J Steenbergen, Wolter Ten Hoeve, Henk M Janssen, Arthur H A M van Onzen, Peter J Hudson, Marc S Robillard
Current antibody-drug conjugates (ADCs) target internalising receptors on cancer cells leading to intracellular drug release. Typically, only a subset of patients with solid tumours has sufficient expression of such a receptor, while there are suitable non-internalising receptors and stroma targets. Here, we demonstrate potent therapy in murine tumour models using a non-internalising ADC that releases its drugs upon a click reaction with a chemical activator, which is administered in a second step. This was enabled by the development of a diabody-based ADC with a high tumour uptake and very low retention in healthy tissues, allowing systemic administration of the activator 2 days later, leading to efficient and selective activation throughout the tumour...
May 4, 2018: Nature Communications
https://www.readbyqxmd.com/read/29723131/insulin-acts-as-a-repressive-factor-to-inhibit-the-ability-of-par2-to-induce-islet-cell-transdifferentiation
#8
Seung-Hee Lee, Ergeng Hao, David Scharp, Fred Levine
Recently, we showed that pancreatitis in the context of profound β-cell deficiency was sufficient to induce islet cell transdifferentiation. In some circumstances, this effect was sufficient to result in recovery from severe diabetes. More recently, we showed that the molecular mechanism by which pancreatitis induced β-cell neogenesis by transdifferentiation was activation of an atypical GPCR called Protease-Activated Receptor 2 (PAR2). However, the ability of PAR2 to induce transdifferentiation occurred only in the setting of profound β-cell deficiency, implying the existence of a repressive factor from those cells...
May 3, 2018: Islets
https://www.readbyqxmd.com/read/29717768/breviscapine-ameliorates-ccl4%C3%A2-induced-liver-injury-in-mice-through-inhibiting-inflammatory-apoptotic-response-and-ros-generation
#9
Yu Liu, Pei-Hao Wen, Xin-Xue Zhang, Yang Dai, Qiang He
Acute liver injury is characterized by fibrosis, inflammation and apoptosis, leading to liver failure, cirrhosis or cancer and affecting the clinical outcome in the long term. However, no effective therapeutic strategy is currently available. Breviscapine, a mixture of flavonoid glycosides, has been reported to have multiple biological functions. The present study aimed to investigate the effects of breviscapine on acute liver injury induced by CCl4 in mice. C57BL/6 mice were subjected to intraperitoneal injection with CCl4 for 8 weeks with or without breviscapine (15 or 30 mg/kg)...
May 2, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29717160/transcriptional-profiling-of-somatostatin-interneurons-in-the-spinal-dorsal-horn
#10
Alexander Chamessian, Michael Young, Yawar Qadri, Temugin Berta, Ru-Rong Ji, Thomas Van de Ven
The spinal dorsal horn (SDH) is comprised of distinct neuronal populations that process different somatosensory modalities. Somatostatin (SST)-expressing interneurons in the SDH have been implicated specifically in mediating mechanical pain. Identifying the transcriptomic profile of SST neurons could elucidate the unique genetic features of this population and enable selective analgesic targeting. To that end, we combined the Isolation of Nuclei Tagged in Specific Cell Types (INTACT) method and Fluorescence Activated Nuclei Sorting (FANS) to capture tagged SST nuclei in the SDH of adult male mice...
May 1, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29713744/skin-neurogenic-inflammation
#11
REVIEW
Jae Eun Choi, Anna Di Nardo
The epidermis closely interacts with nerve endings, and both epidermis and nerves produce substances for mutual sustenance. Neuropeptides, like substance P (SP) and calcitonin gene-related protein (CGRP), are produced by sensory nerves in the dermis; they induce mast cells to release vasoactive amines that facilitate infiltration of neutrophils and T cells. Some receptors are more important than others in the generation of itch. The Mas-related G protein-coupled receptors (Mrgpr) family as well as transient receptor potential ankyrin 1 (TRPA1) and protease activated receptor 2(Par2) have important roles in itch and inflammation...
April 30, 2018: Seminars in Immunopathology
https://www.readbyqxmd.com/read/29713059/inactivation-of-the-serine-protease-htra1-inhibits-tumor-growth-by-deregulating-angiogenesis
#12
Ralph Klose, M Gordian Adam, Eva-Maria Weis, Iris Moll, Joycelyn Wüstehube-Lausch, Fabian Tetzlaff, Chio Oka, Michael Ehrmann, Andreas Fischer
The serine protease HTRA1 is involved in several vascular diseases and its expression is often deregulated in cancer. We aimed at identifying how HTRA1 in the vasculature affects tumor growth. Here we report that silencing of HTRA1 in cultured endothelial cells increased migration rate and tube formation, whereas forced HTRA1 expression impaired sprouting angiogenesis. Mechanistically, endothelial HTRA1 expression enhanced Delta/Notch signaling by reducing the amount of the weak Notch ligand JAG1. HTRA1 physically interacted with JAG1 and cleaved it within the intracellular domain, leading to protein degradation...
May 1, 2018: Oncogene
https://www.readbyqxmd.com/read/29709935/use-of-nasopancreatic-drainage-for-severe-post-endoscopic-retrograde-cholangiopancreatography-pancreatitis-a-case-series
#13
Shinya Kawaguchi, Masataka Kikuyama, Tatsunori Satoh, Shuzo Terada
Five patients complaining of severe pain due to severe post-endoscopic retrograde cholangiopancreatography pancreatitis (PEP) underwent nasopancreatic drainage (NPD) placement. Pain relief was achieved on the second, fourth, and fifth day in three, one, and one patients, respectively. Four patients underwent pancreatic juice culture; all were positive. Our results suggest that NPD can relieve severe PEP with severe pain. Bacteria-induced protease-activated receptor-2 activation may be associated with PEP.
April 27, 2018: Internal Medicine
https://www.readbyqxmd.com/read/29709920/impairment-of-protease-activated-receptor-2-induced-relaxation-of-aortas-of-aged-spontaneously-hypertensive-rat
#14
Makoto Ando, Takayuki Matsumoto, Shota Kobayashi, Maika Iguchi, Kumiko Taguchi, Tsuneo Kobayashi
Hypertension is one of the most prevalent diseases worldwide and can cause harmful complications within the vascular system. Further research on vascular responsiveness to different ligands and diverse receptors in various arteries is required to understand the mechanisms underlying the development of these vascular complications. Here, we investigated the vasorelaxant effect of the protease-activated receptor 2 (PAR2) agonist 2-furoyl-LIGRLO-amide (2-Fly) and two commonest agents, namely endothelium-dependent dilator acetylcholine (ACh) and endothelium-independent dilator sodium nitroprusside (SNP), on the thoracic aorta isolated from aged spontaneously hypertensive rats (SHR) (age, 52±1 weeks)...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29705335/molecular-mechanisms-of-platelet-activation-and-aggregation-induced-by-breast-cancer-cells
#15
Marta Zarà, Ilaria Canobbio, Caterina Visconte, Jessica Canino, Mauro Torti, Gianni Francesco Guidetti
Tumor cell-induced platelet aggregation represents a critical process both for successful metastatic spread of the tumor and for the development of thrombotic complications in cancer patients. To get further insights into this process, we investigated and compared the molecular mechanisms of platelet aggregation induced by two different breast cancer cell lines (MDA-MB-231 and MCF7) and a colorectal cancer cell line (Caco-2). All the three types of cancer cells were able to induce comparable platelet aggregation, which, however, was observed exclusively in the presence of CaCl2 and autologous plasma...
April 26, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29704879/topical-retinol-attenuates-stress-induced-aging-signs-in-human-skin-ex-vivo-through-egfr-activation-via-egf-but-not-erk-and-ap-1-activation
#16
Bruna Romana-Souza, Welker Silva-Xavier, Andréa Monte-Alto-Costa
Stress-induced oxidative damage and the inflammatory response lead to degradation of collagen and elastic fibers and wrinkle formation. Topical retinol (or vitamin A) can be a strategy to attenuate the effects of stress in skin since it promotes collagen and elastic fiber production and reduces protease synthesis. This study investigated the effect of topical retinol in stressed human skin using in vivo and ex vivo models. Human skin explants were treated with high levels of epinephrine (as observed in stressed patients) and topically with retinol for 13 days...
April 28, 2018: Experimental Dermatology
https://www.readbyqxmd.com/read/29700120/protease-activated-receptor-2-plays-a-critical-role-in-vascular-inflammation-and-atherosclerosis-in-apolipoprotein-e-deficient-mice
#17
Tomoya Hara, Pham Tran Phuong, Daiju Fukuda, Koji Yamaguchi, Chie Murata, Sachiko Nishimoto, Shusuke Yagi, Kenya Kusunose, Hirotsugu Yamada, Takeshi Soeki, Tetsuzo Wakatsuki, Issei Imoto, Michio Shimabukuro, Masataka Sata
Background -The coagulation system is closely linked with vascular inflammation, although the underlying mechanisms are still obscure. Recent studies show that protease-activated receptor (PAR)-2, a major receptor of activated factor X (FXa), are expressed in both vascular cells and leukocytes, suggesting that PAR-2 may contribute to the pathogenesis of inflammatory diseases. Here we investigated the role of PAR-2 in vascular inflammation and atherogenesis. Methods -We generated apolipoprotein E-deficient ( ApoE-/- ) mice lacking systemic PAR-2 expression ( ApoE-/- PAR-2-/- )...
April 26, 2018: Circulation
https://www.readbyqxmd.com/read/29695020/significant-hypo-responsiveness-to-gpvi-and-clec-2-agonists-in-pre-term-and-full-term-neonatal-platelets-and-following-immune-thrombocytopenia
#18
Alexander T Hardy, Verónica Palma-Barqueros, Stephanie K Watson, Jean-Daniel Malcor, Johannes A Eble, Elizabeth E Gardiner, José E Blanco, Rafael Guijarro-Campillo, Juan L Delgado, María L Lozano, Raúl Teruel-Montoya, Vicente Vicente, Steve P Watson, José Rivera, Francisca Ferrer-Marín
Neonatal platelets are hypo-reactive to the tyrosine kinase-linked receptor agonist collagen. Here, we have investigated whether the hypo-responsiveness is related to altered levels of glycoprotein VI (GPVI) and integrin α2β1, or to defects in downstream signalling events by comparison to platelet activation by C-type lectin-like receptor 2 (CLEC-2). GPVI and CLEC-2 activate a Src- and Syk-dependent signalling pathway upstream of phospholipase C (PLC) γ2. Phosphorylation of a conserved YxxL sequence known as a (hemi) immunotyrosine-based-activation-motif (ITAM) in both receptors is critical for Syk activation...
April 25, 2018: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/29685684/characterization-of-protease-activated-receptor-par-ligands-parmodulins-are-reversible-allosteric-inhibitors-of-par1-driven-calcium-mobilization-in-endothelial-cells
#19
Disha M Gandhi, Mark W Majewski, Ricardo Rosas, Kaitlin Kentala, Trevor J Foster, Eric Greve, Chris Dockendorff
Several classes of ligands for Protease-Activated Receptors (PARs) have shown impressive anti-inflammatory and cytoprotective activities, including PAR2 antagonists and the PAR1-targeting parmodulins. In order to support medicinal chemistry studies with hundreds of compounds and to perform detailed mode-of-action studies, it became important to develop a reliable PAR assay that is operational with endothelial cells, which mediate the cytoprotective effects of interest. We report a detailed protocol for an intracellular calcium mobilization assay with adherent endothelial cells in multiwell plates that was used to study a number of known and new PAR1 and PAR2 ligands, including an alkynylated version of the PAR1 antagonist RWJ-58259 that is suitable for the preparation of tagged or conjugate compounds...
April 6, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29677491/the-allergen-der-p3-from-house-dust-mite-stimulates-store-operated-ca-2-channels-and-mast-cell-migration-through-par4-receptors
#20
Yu-Ping Lin, Charmaine Nelson, Holger Kramer, Anant B Parekh
The house dust mite is the principal source of perennial aeroallergens in man. How these allergens activate innate and adaptive immunity is unclear, and therefore, there are no therapies targeting mite allergens. Here, we show that house dust mite extract activates store-operated Ca2+ channels, a common signaling module in numerous cell types in the lung. Activation of channel pore-forming Orai1 subunits by mite extract requires gating by STIM1 proteins. Although mite extract stimulates both protease-activated receptor type 2 (PAR2) and PAR4 receptors, Ca2+ influx is more tightly coupled to the PAR4 pathway...
April 19, 2018: Molecular Cell
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