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Protease activated receptor 2

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https://www.readbyqxmd.com/read/28198394/cockroach-protease-allergen-induces-allergic-airway-inflammation-via-epithelial-cell-activation
#1
Sagar L Kale, Komal Agrawal, Shailendra Nath Gaur, Naveen Arora
Protease allergens are known to enhance allergic inflammation but their exact role in initiation of allergic reactions at mucosal surfaces still remains elusive. This study was aimed at deciphering the role of serine protease activity of Per a 10, a major cockroach allergen in initiation of allergic inflammation at mucosal surfaces. We demonstrate that Per a 10 increases epithelial permeability by disruption of tight junction proteins, ZO-1 and occludin, and enhances the migration of Monocyte derived dendritic cell precursors towards epithelial layer as exhibited by trans-well studies...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28191683/immediate-type-allergic-and-protease-mediated-reactions-are-involved-in-scratching-behavior-induced-by-topical-application-of-dermatophagoides-farinae-extract-in-nc-nga-mice
#2
Yoshihito Yamada, Yuhki Ueda, Aki Nakamura, Shoji Kanayama, Rie Tamura, Kei Hashimoto, Tatsumi Matsumoto, Ritsuko Ishii
Atopic dermatitis (AD)-like dermatitis can be induced by repeated topical application of an ointment containing Dermatophagoides farinae body (Dfb) extract in NC/Nga mice. This AD-like murine model also exhibits a biphasic increase in the number of scratching behavior after topical application of Dfb ointment. In this study, we investigated the possible mechanisms underlying the scratching behavior in each phase. An increase in the content of mast cell derived mediators such as histamine and 5-hydroxytryptamine in the lesional skin and increased vascular permeability were observed in the early phase after the Dfb ointment application...
February 13, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28179423/xanthine-dehydrogenase-1-silencing-in-aedes-aegypti-mosquitoes-promotes-a-blood-feeding-induced-adulticidal-activity
#3
Jun Isoe, Natthida Petchampai, Yurika E Isoe, Katrina Co, Stacy Mazzalupo, Patricia Y Scaraffia
Aedesaegypti has 2 genes encoding xanthine dehydrogenase (XDH). We analyzed XDH1 and XDH2 gene expression by real-time quantitative PCR in tissues from sugar- and blood-fed females. Differential XDH1 and XDH2 gene expression was observed in tissues dissected throughout a time course. We next exposed females to blood meals supplemented with allopurinol, a well-characterized XDH inhibitor. We also tested the effects of injecting double-stranded RNA (dsRNA) against XDH1, XDH2, or both. Disruption of XDH by allopurinol or XDH1 by RNA interference significantly affected mosquito survival, causing a disruption in blood digestion, excretion, oviposition, and reproduction...
February 8, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28169521/biased-signaling-by-peptide-agonists-of-protease-activated-receptor-2
#4
Yuhong Jiang, Mei-Kwan Yau, W Mei Kok, Junxian Lim, Kai-Chen Wu, Ligong Liu, Timothy A Hill, Jacky Y Suen, David P Fairlie
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 intracellular signaling pathways. There are no synthetic PAR2 ligands that reproduce the same signaling profiles and potencies as proteases. Structure-activity relationships here for 26 compounds spanned a signaling bias over 3 log units, culminating in three small ligands as biased agonist tools for interrogating PAR2 functions...
February 7, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28162529/-292-protease-activated-receptor-2-par2-is-a-mediator-of-nociception-in-a-mouse-model-of-migraine
#5
S Hassler, T Price, G Dussor, S Boitano, J Vagner
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28160743/dioxolanea3-phosphatidylethanolamines-are-generated-by-human-platelets-and-stimulate-neutrophil-integrin-expression
#6
Maceler Aldrovandi, Christine Hinz, Sarah N Lauder, Helen Podmore, Martin Hornshaw, David A Slatter, Victoria J Tyrrell, Stephen R Clark, Lawrence J Marnett, Peter W Collins, Robert C Murphy, Valerie B O'Donnell
Activated platelets generate an eicosanoid proposed to be 8-hydroxy-9,10-dioxolane A3 (DXA3). Herein, we demonstrate that significant amounts of DXA3 are rapidly attached to phosphatidylethanolamine (PE) forming four esterified eicosanoids, 16:0p, 18:0p, 18:1p and 18:0a/DXA3-PEs that can activate neutrophil integrin expression. These lipids comprise the majority of DXA3 generated by platelets, are formed in ng amounts (24.3±6.1ng/2×10(8)) and remain membrane bound. Pharmacological studies revealed DXA3-PE formation involves cyclooxygenase-1 (COX), protease-activated receptors (PAR) 1 and 4, cytosolic phospholipase A2 (cPLA2), phospholipase C and intracellular calcium...
January 13, 2017: Redox Biology
https://www.readbyqxmd.com/read/28159725/topical-treatments-of-saussurea-costus-root-and-thuja-orientalis-l-synergistically-alleviate-atopic-dermatitis-like-skin-lesions-by-inhibiting-protease-activated-receptor-2-and-nf-%C3%AE%C2%BAb-signaling-in-hacat-cells-and-nc-nga-mice
#7
Hye Jeong Yang, Min Jung Kim, Suna Kang, Na Rang Moon, Da Sol Kim, Na Ra Lee, Kang Sung Kim, Sunmin Park
ETHNOPHARMACOLOGICAL RELEVANCE: The root of Saussurea costus (Aucklandia lappa Decne, Aucklandiae Radix, SC) and Thuja orientalis L. (TOL) have been traditionally used as anti-inflammatory agents in Korea. However, they have not been studied for the efficacy of atopic dermatitis (AD) treatment, a chronic inflammatory skin disease. We investigated the efficacy of topical applications with 1,3-butyleneglycol extracts of SC and TOL to alleviate the symptoms of AD. MATERIALS AND METHODS: HaCaT cells and the dorsal skin of Nc/Nga mice had a local exposure of house mite extracts and 2,4-dinitrochlorobenzene (DNCB), respectively...
January 31, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28150441/characterization-of-the-binding-of-a-glycosylated-serine-protease-from-euphorbia-cf-lactea-latex-to-human-fibrinogen
#8
Jaruwan Siritapetawee, Chutima Talabnin, Jarunee Vanichtanankul, Chomphunuch Songsiriritthigul, Kanjana Thumanu, Chun-Jung Chen, Nantarat Komanasin
In this study, the binding of a glycosylated serine protease (EuP-82) with human fibrinogen was investigated by the isothermal titration calorimetry (ITC). The ITC analysis indicated that the binding of EuP-82 to fibrinogen in the conditions with or without the activator (Ca(2+) ) was an exothermic reaction (dominant negative enthalpy), which tended to be driven by hydrogen bonding and van der Waals interactions. In contrast, the binding of fibrinogen-EuP-82 in the condition with the inhibitor (Zn(2+) ) was an unfavorable endothermic reaction...
February 1, 2017: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/28148395/tissue-factor-factor-viia-complex-triggers-protease-activated-receptor-2-dependent-growth-factor-release-and-migration-in-ovarian-cancer
#9
Alice Chanakira, Pamela R Westmark, Irene M Ong, John P Sheehan
OBJECTIVE: Enhanced tissue factor (TF) expression in epithelial ovarian cancer (EOC) is associated with aggressive disease. Our objective was to evaluate the role of the TF-factor VIIa-protease-activated receptor-2 (PAR-2) pathway in human EOC. METHODS: TCGA RNAseq data from EOC databases were analyzed for PAR expression. Cell and microparticle (MP) associated TF protein expression (Western blot) and MP-associated coagulant activity were determined in human EOC (SKOV-3, OVCAR-3 and CaOV-3) and control cell lines...
January 29, 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/28146220/par-2-expression-in-the-gingival-crevicular-fluid-reflects-chronic-periodontitis-severity
#10
Henrique Fukushima, Vanessa Tubero Euzebio Alves, Verônica Franco de Carvalho, Lucas Macedo Batitucci Ambrósio, Rosangela Aparecida Dos Santos Eichler, Maria Helena Catelli de Carvalho, Luciana Saraiva, Marinella Holzhausen
Recent studies investigating protease-activated receptor type 2 (PAR-2) suggest an association between the receptor and periodontal inflammation. It is known that gingipain, a bacterial protease secreted by the important periodontopathogen Porphyromonas gingivalis can activate PAR-2. Previous studies by our group found that PAR-2 is overexpressed in the gingival crevicular fluid (GCF) of patients with moderate chronic periodontitis (MP). The present study aimed at evaluating whether PAR-2 expression is associated with chronic periodontitis severity...
January 26, 2017: Brazilian Oral Research
https://www.readbyqxmd.com/read/28126338/usp15-attenuates-igf-i-signaling-by-antagonizing-nedd4-induced-irs-2-ubiquitination
#11
Toshiaki Fukushima, Hidehito Yoshihara, Haruka Furuta, Fumihiko Hakuno, Yasushi Saeki, Shun-Ichiro Iemura, Tohru Natsume, Yusuke Nakatsu, Hideaki Kamata, Tomoichiro Asano, Masayuki Komada, Shin-Ichiro Takahashi
Insulin receptor substrates (IRSs) are phosphorylated by IGF-I receptor tyrosine kinase in a ligand-dependent manner. In turn, they bind to and activate effector proteins such as PI3K, leading to various cell responses including cell proliferation. We had reported that ubiquitin ligase Nedd4 induces mono-ubiquitination of IRS-2, thereby enhancing IRS-2 tyrosine phosphorylation, leading to increased IGF signaling and mitogenic activity. Here we show that ubiquitin-specific protease 15 (USP15) antagonizes the effect of Nedd4 on IRS-2...
January 23, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28126288/medicinal-attributes-of-1-2-3-triazoles-current-developments
#12
REVIEW
Divya Dheer, Virender Singh, Ravi Shankar
1,2,3-Triazoles are important five-membered heterocyclic scaffold due to their extensive biological activities. This framework can be readily obtained in good to excellent yields on the multigram scale through click chemistry via reaction of aryl/alkyl halides, alkynes and NaN3 under ambient conditions. It has been an emerging area of interest for many researchers throughout the globe owing to its immense pharmacological scope. The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors (celecoxib, pyrazofurin), HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials...
January 18, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28109095/-establishment-of-a-sd-rat-model-of-vulvar-lichen-simplex-chronicus-and-detection-of-the-expression-of-protease-activated-receptor-2
#13
Huan Yang, Zhen-Hua Fu, Hua-Jun Tang, Cheng-Zhi Li
OBJECTIVE: To establish a SD rat model of vulvar lichen simplex chronicus (LSC) and investigate the expression of protease activated receptor 2 (PAR2) in the genital skin. METHODS: Seventy female SD rats were randomly divided into group A (blank control group, n=10), group B (with application of acetone solution 3 times per week for 10 weeks, n=10), group C (with chronic mechanical irritation 3 times per week for 10 weeks, n=10), and group D (with topical treatment with 0...
January 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28103056/age-related-changes-to-vascular-protease-activated-receptor-2-in-metabolic-syndrome-a-relationship-between-oxidative-stress-receptor-expression-and-endothelium-dependent-vasodilation
#14
Kana Maruyama, Satomi Kagota, John J McGuire, Hirokazu Wakuda, Noriko Yoshikawa, Kazuki Nakamura, Kazumasa Shinozuka
Protease-activated receptor 2 (PAR2) is expressed in vascular endothelium. Nitric oxide (NO) - cyclic GMP-mediated vasodilation in response to 2-furoyl-LIGRLO-amide (2fLIGRLO), a PAR2-activating peptide, is impaired in aortas from aged SHRSP.Z-Lepr(fa)/IzmDmcr (SHRSP.ZF) rats with metabolic syndrome. Here we investigated mechanisms linking PAR2's vascular effects to phenotypic characteristics of male SHRSP.ZF rats at 10, 20, and 30 weeks of age. We found vasodilation responses to either 2fLIGRLO or enzyme-mediated PAR2 activation by trypsin were sustained until 20 weeks and lessened at 30 weeks...
October 19, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28096305/epithelial-expression-and-function-of-trypsin-3-in-irritable-bowel-syndrome
#15
Claire Rolland-Fourcade, Alexandre Denadai-Souza, Carla Cirillo, Cintya Lopez, Josue Obed Jaramillo, Cleo Desormeaux, Nicolas Cenac, Jean-Paul Motta, Muriel Larauche, Yvette Taché, Pieter Vanden Berghe, Michel Neunlist, Emmanuel Coron, Sylvain Kirzin, Guillaume Portier, Delphine Bonnet, Laurent Alric, Stephen Vanner, Celine Deraison, Nathalie Vergnolle
OBJECTIVES: Proteases are key mediators of pain and altered enteric neuronal signalling, although the types and sources of these important intestinal mediators are unknown. We hypothesised that intestinal epithelium is a major source of trypsin-like activity in patients with IBS and this activity signals to primary afferent and enteric nerves and induces visceral hypersensitivity. DESIGN: Trypsin-like activity was determined in tissues from patients with IBS and in supernatants of Caco-2 cells stimulated or not...
January 17, 2017: Gut
https://www.readbyqxmd.com/read/28064059/par1-activation-affects-the-neurotrophic-properties-of-schwann-cells
#16
Elena Pompili, Cinzia Fabrizi, Francesca Somma, Virginia Correani, Bruno Maras, Maria Eugenia Schininà, Viviana Ciraci, Marco Artico, Francesco Fornai, Lorenzo Fumagalli
Protease-activated receptor-1 (PAR1) is the prototypic member of a family of four G-protein-coupled receptors that signal in response to extracellular proteases. In the peripheral nervous system, the expression and/or the role of PARs are still poorly investigated. High PAR1 mRNA expression was found in the rat dorsal root ganglia and the signal intensity of PAR1 mRNA increased in response to sciatic nerve transection. In the sciatic nerve, functional PAR1 receptor was reported at the level of non-compacted Schwann cell myelin microvilli of the nodes of Ranvier...
January 4, 2017: Molecular and Cellular Neurosciences
https://www.readbyqxmd.com/read/28063023/vorapaxar-the-current-role-and-future-directions-of-a-novel-protease-activated-receptor-antagonist-for-risk-reduction-in-atherosclerotic-disease
#17
REVIEW
Rebecca J Gryka, Leo F Buckley, Sarah M Anderson
INTRODUCTION: Despite the current standard of care, patients with cardiovascular disease remain at a high risk for recurrent events. Inhibition of thrombin-mediated platelet activation through protease-activated receptor-1 antagonism may provide reductions in atherosclerotic disease beyond those achievable with the current standard of care. OBJECTIVE: Our primary objective is to evaluate the clinical literature regarding the role of vorapaxar (Zontivity™) in the reduction of cardiovascular events in patients with a history of myocardial infarction and peripheral artery disease...
January 6, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28055299/guiding-bispecific-monovalent-antibody-formation-through-proteolysis-of-igg1-single-chain
#18
Nazzareno Dimasi, Ryan Fleming, Kris F Sachsenmeier, Binyam Bezabeh, Carl Hay, Jincheng Wu, Erin Sult, Saravanan Rajan, Li Zhuang, Peter Cariuk, Andrew Buchanan, Michael A Bowen, Herren Wu, Changshou Gao
We developed an IgG1 domain-tethering approach to guide the correct assembly of two light and two heavy chains, derived from two different antibodies, to form bispecific monovalent antibodies in IgG1 format. We show here that assembling two different light and heavy chains by sequentially connecting them with protease-cleavable polypeptide linkers results in the generation of monovalent bispecific antibodies that have IgG1 sequence, structure and functional properties. This approach was used to generate a bispecific monovalent antibody targeting the epidermal growth factor receptor and the type I insulin-like growth factor receptor that: 1) can be produced and purified using standard IgG1 techniques; 2) exhibits stability and structural features comparable to IgG1; 3) binds both targets simultaneously; and 4) has potent anti-tumor activity...
January 5, 2017: MAbs
https://www.readbyqxmd.com/read/28052875/liver-x-receptor-%C3%AE-lxr%C3%AE-increases-aqp2-protein-level-via-a-post-transcriptional-mechanism-in-renal-collecting-ducts
#19
Wen Su, Shi-Zheng Huang, Min Gao, Xiao-Mu Kong, Jan-Ake Gustafsson, Su-Juan Xu, Bing Wang, Feng Zheng, Li-Hong Chen, Nan-Ping Wang, You-Fei Guan, Xiao-Yan Zhang
Liver X Receptors (LXRs) including LXRα and LXRβ are nuclear receptor transcription factors and play an important role in lipid and glucose metabolism. It has been previously reported that mice lacking LXRβ but not LXRα develop a severe urine concentrating defect, likely via a central mechanism. Here we provide evidence that LXRβ regulates water homeostasis through increasing aquaporin 2 (AQP2) protein levels in renal collecting ducts. LXRβ-/- mice exhibited a reduced response to dDAVP stimulation, suggesting that the diabetes insipidus phenotype is of both central and nephrogenic origin...
January 4, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28035779/reduction-of-intracerebral-hemorrhage-by-rivaroxaban-after-tpa-thrombolysis-is-associated-with-downregulation-of-par-1-and-par-2
#20
Ryuta Morihara, Toru Yamashita, Syoichiro Kono, Jingwei Shang, Yumiko Nakano, Kota Sato, Nozomi Hishikawa, Yasuyuki Ohta, Stefan Heitmeier, Elisabeth Perzborn, Koji Abe
This study aimed to assess the risk of intracerebral hemorrhage (ICH) after tissue-type plasminogen activator (tPA) treatment in rivaroxaban compared with warfarin-pretreated male Wistar rat brain after ischemia in relation to activation profiles of protease-activated receptor-1, -2, -3, and -4 (PAR-1, -2, -3, and -4). After pretreatment with warfarin (0.2 mg/kg/day), low-dose rivaroxaban (60 mg/kg/day), high-dose rivaroxaban (120 mg/kg/day), or vehicle for 14 days, transient middle cerebral artery occlusion was induced for 90 min, followed by reperfusion with tPA (10 mg/kg/10 ml)...
December 30, 2016: Journal of Neuroscience Research
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