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Protease activated receptor 2

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https://www.readbyqxmd.com/read/28064059/par1-activation-affects-the-neurotrophic-properties-of-schwann-cells
#1
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
#2
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
#3
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
#4
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
#5
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
https://www.readbyqxmd.com/read/28035371/the-anti-metastatic-effects-of-the-phytoestrogen-arctigenin-on-human-breast-cancer-cell-lines-regardless-of-the-status-of-er-expression
#6
Thressi Maxwell, So-Young Chun, Kyu-Shik Lee, Soyoung Kim, Kyung-Soo Nam
Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In spite of the health benefits of phytoestrogens reducing the risk of osteoporosis, heart disease, and menopausal symptoms, its benefits against the risk of breast cancer have not been fully elucidated. Thus, we investigated the effects of arctigenin on metastasis of breast cancer using both estrogen receptor (ER)-positive MCF-7 and ER-negative MDA-MB-231 human breast cancer cell lines to see if the effects are dependent on the status of ER expression...
December 29, 2016: International Journal of Oncology
https://www.readbyqxmd.com/read/28030866/increase-of-mast-cell-nerve-association-and-neuropeptide-receptor-expression-on-mast-cells-in-perennial-allergic-rhinitis
#7
Duc Dung Le, David Schmit, Sebastian Heck, Albert Joachim Omlor, Martina Sester, Christian Herr, Bernhard Schick, François Daubeuf, Sebastian Fähndrich, Robert Bals, Nelly Frossard, Basel Al Kadah, Quoc Thai Dinh
OBJECTIVES: Mast cells (MCs) and nerves play an important role in allergic rhinitis (AR), but little is known about their crosstalk in AR. The aim of this study was to investigate MC-nerve interaction in the human nasal mucosa during AR. METHODS: The association between MCs and nerves, the expression of neuropeptide receptors (neurokinin 1 receptor [NK1R], neurokinin 2 receptor [NK2R], calcitonin gene-related peptide receptor [CGRPR], and MrgX2) on MCs, and protease-activated receptor 2 (PAR2) and tyrosine receptor kinase A (TrkA) on nerve fibres in the human nasal mucosa were investigated with immunofluorescence and real-time PCR...
December 29, 2016: Neuroimmunomodulation
https://www.readbyqxmd.com/read/28025140/protease-activated-receptor-2-exacerbates-adenine-induced-renal-tubulointerstitial-injury-in-mice
#8
Sakiko Hayashi, Yuji Oe, Tomofumi Fushima, Emiko Sato, Hiroshi Sato, Sadayoshi Ito, Nobuyuki Takahashi
Hypercoagulability is associated with chronic kidney disease (CKD). Tissue factor/factor VIIa complex and factor Xa in the coagulation cascade are known to activate protease-activated receptor 2 (PAR2), and to cause inflammation and tissue injury. Although PAR2 is highly expressed in the kidney, it is unclear whether PAR2 plays a pathogenic role in CKD. To test this, we fed the mice lacking Par2 (F2rl1(-/-)) and wild type (F2rl1(+/+)) mice with adenine diet to induce tubulointerstitial injury, a hallmark of CKD...
December 23, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28011482/galectin-3-is-implicated-in-tumor-progression-and-resistance-to-anti-androgen-drug-through-regulation-of-androgen-receptor-signaling-in-prostate-cancer
#9
Tsogt-Ochir Dondoo, Tomoharu Fukumori, Kei Daizumoto, Tomoya Fukawa, Miho Kohzuki, Minoru Kowada, Yoshito Kusuhara, Hidehisa Mori, Hiroyoshi Nakatsuji, Masayuki Takahashi, Hiro-Omi Kanayama
BACKGROUND: Castration-resistant prostate cancer (CRPC)-related deaths are increasing worldwide. Therefore, clarification of the mechanisms of hormone-related tumor progression and resistance to anti-androgen drugs is useful in order to develop strategies for appropriate treatment of CRPC. Galectin-3 has been shown to be correlated with tumor progression in a variety of cancer types through the regulation of tumor proliferation, angiogenesis, and apoptosis. MATERIALS AND METHODS: We examined tumor cell invasion and migration using the xCELLigence system...
January 2017: Anticancer Research
https://www.readbyqxmd.com/read/27999370/effect-of-lead-pb-on-inflammatory-processes-in-the-brain
#10
REVIEW
Karina Chibowska, Irena Baranowska-Bosiacka, Anna Falkowska, Izabela Gutowska, Marta Goschorska, Dariusz Chlubek
That the nervous system is the main target of lead (Pb) has long been considered an established fact until recent evidence has linked the Pb effect on the immune system to the toxic effects of Pb on the nervous system. In this paper, we present recent literature reports on the effect of Pb on the inflammatory processes in the brain, particularly the expression of selected cytokines in the brain (interleukin 6, TGF-β1, interleukin 16, interleukin 18, and interleukin 10); expression and activity of enzymes participating in the inflammatory processes, such as cyclooxygenase 2, caspase 1, nitrogen oxide synthase (NOS 2) and proteases (carboxypeptidases, metalloproteinases and chymotrypsin); and the expression of purine receptors P2X4 and P2X7...
December 19, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27998795/mechanisms-of-modulation-of-brain-microvascular-endothelial-cells-function-by-thrombin
#11
Eugen Brailoiu, Megan M Shipsky, Guang Yan, Mary E Abood, G Cristina Brailoiu
Brain microvascular endothelial cells are a critical component of the blood-brain barrier. They form a tight monolayer which is essential for maintaining the brain homeostasis. Blood-derived proteases such as thrombin may enter the brain during pathological conditions like trauma, stroke, and inflammation and further disrupts the permeability of the blood-brain barrier, via incompletely characterized mechanisms. We examined the underlying mechanisms evoked by thrombin in rat brain microvascular endothelial cells (RBMVEC)...
December 17, 2016: Brain Research
https://www.readbyqxmd.com/read/27995367/paracoccidioides-brasiliensis-induces-cytokine-secretion-in-epithelial-cells-in-a-protease-activated-receptor-dependent-par-manner
#12
Priscila de Oliveira, Maria Aparecida Juliano, Aparecida Sadae Tanaka, Adriana Karaoglanovic Carmona, Saara Maria Batista Dos Santos, Bianca Carla Silva Campitelli de Barros, Paloma Korehisa Maza, Rosana Puccia, Erika Suzuki
Paracoccidioides brasiliensis is one of the etiological agents of the human systemic mycosis paracoccidioidomycosis. Protease-activated receptors (PARs) are expressed in many cell types and comprise a family of G protein-coupled receptors (PAR-1, PAR-2, and PAR-4), which may be activated by proteases secreted by several pathogens. In the present study, we showed that the pathogenic fungus P. brasiliensis secretes components that promote interleukin (IL)-6 and IL-8 secretion by the lung epithelial cell line A549...
December 19, 2016: Medical Microbiology and Immunology
https://www.readbyqxmd.com/read/27993717/mapping-transmembrane-residues-of-proteinase-activated-receptor-2-par2-that-influence-ligand-modulated-calcium-signaling
#13
J Y Suen, M N Adams, J Lim, P K Madala, W Xu, A Cotterell, Y He, Mei-Kwan Yau, J D Hooper, D P Fairlie
Proteinase-activated receptor 2 (PAR2) is a G protein-coupled receptor involved in metabolism, inflammation, and cancers. It is activated by proteolysis, which exposes a nascent N-terminal sequence that becomes a tethered agonist. Short synthetic peptides corresponding to this sequence also activate PAR2, while small organic molecules show promising PAR2 antagonism. Developing PAR2 ligands into pharmaceuticals is hindered by a lack of knowledge of how synthetic ligands interact with and differentially modulate PAR2...
December 16, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27987367/activation-of-matrix-metalloproteinase-mmp-9-by-membrane-type-1-matrix-metalloproteinase-mmp-2-axis-stimulates-tumor-metastasis
#14
Zichen Li, Takahisa Takino, Yoshio Endo, Hiroshi Sato
An artificial receptor for pro-matrix metalloproteinase-9 (proMMP-9) was created by fusing tissue inhibitor of MMP-1 (TIMP-1) with type II transmembrane mosaic serine protease (MSP-T1). Expression of MSP-T1 in 293T cells induced binding of proMMP-9, which was processed by MMP-2 activated by Membrane-Type-1 MMP (MT1-MMP). HT1080 cells transfected with MSP-T1 gene produced activated MMP-9 in collagen gel, and addition of proMMP-2 to the culture augmented it, which resulted in intensive collagen digestion. These cells metastasized into chick embryonic liver more than control cells...
December 17, 2016: Cancer Science
https://www.readbyqxmd.com/read/27981668/activation-of-protease-activated-receptor-2-mediates-cutaneous-vasodilatation-but-not-sweating-roles-of-nitric-oxide-synthase-and-cyclooxygenase
#15
Naoto Fujii, Brendan D McNeely, Sarah Y Zhang, Yasmine C Abdellaoui, Mercy O Danquah, Glen P Kenny
Protease-activated receptor 2 (PAR2) is present in human skin including keratinocytes, endothelial cells of skin microvessels, and eccrine sweat glands. However, whether PAR2 functionally contributes to the regulation of cutaneous blood flow and sweating remains entirely unclear in humans in vivo. We hypothesized that activation of PAR2 directly stimulates cutaneous vasodilatation and sweating via actions of nitric oxide synthase (NOS) and cyclooxygenase (COX). In twelve physically active young males (29 ± 5 years), cutaneous vascular conductance (CVC) and sweat rate were measured at four intradermal microdialysis forearm skin sites that were treated with 1) lactated Ringer's solution (Control), 2) 10 mm N(ω) -nitro-L -arginine (NOS inhibitor), 3) 10 mm ketorolac (COX inhibitor), or 4) a combination of both inhibitors...
December 16, 2016: Experimental Physiology
https://www.readbyqxmd.com/read/27965452/bystander-host-cell-killing-effects-of-clostridium-perfringens-enterotoxin
#16
Archana Shrestha, Matthew R Hendricks, Jennifer M Bomberger, Bruce A McClane
: Clostridium perfringens enterotoxin (CPE) binds to claudin receptors, e.g., claudin-4, and then forms a pore that triggers cell death. Pure cultures of host cells that do not express claudin receptors, e.g., fibroblasts, are unaffected by pathophysiologically relevant CPE concentrations in vitro However, both CPE-insensitive and CPE-sensitive host cells are present in vivo Therefore, this study tested whether CPE treatment might affect fibroblasts when cocultured with CPE-sensitive claudin-4 fibroblast transfectants or Caco-2 cells...
December 13, 2016: MBio
https://www.readbyqxmd.com/read/27965128/anti-angiogenic-potential-of-trypsin-inhibitor-purified-from-cucumis-melo-seeds-homology-modeling-and-molecular-docking-perspective
#17
Hassan Rasouli, Sharham Parvaneh, Azadeh Mahnam, Mohsen Rastegari-Pouyani, Zohreh Hoseinkhani, Kamran Mansouri
Melons have a good source of protease inhibitors. Its fruit and seeds have been used as a traditional medicine. However, its effects on angiogenesis and mechanism of its action remain elusive. Herein trypsin inhibitor from aqueous extract of C. melo seeds (TICMS) was purified. Its effects on different steps of angiogenesis were evaluated. Also, we examined its effects on migration and angiogenesis of endothelial cells. Three dimensional model of TICMS protein was accurately built in which TICMS docked to αVβ3 integrin and VEGFR1...
December 10, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27959396/ulinastatin-post-treatment-attenuates-lipopolysaccharide-induced-acute-lung-injury-in-rats-and-human-alveolar-epithelial-cells
#18
Yunpeng Luo, Wen Che, Mingyan Zhao
Ulinastatin (UTI), a serine protease inhibitor, possesses anti-inflammatory properties and has been suggested to modulate lipopolysaccharide (LPS)-induced acute lung injury (ALI). High-mobility group box 1 (HMGB1), a nuclear DNA-binding protein, plays a key role in the development of ALI. The aim of this study was to investigate whether UTI attenuates ALI through the inhibition of HMGB1 expression and to elucidate the underlying molecular mechanisms. ALI was induced in male rats by the intratracheal instillation of LPS (5 mg/kg)...
December 13, 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/27925497/anti-inflammatory-and-anticancer-effects-of-flavonol-glycosides-from-diplotaxis-harra-through-gsk3%C3%AE-regulation-in-intestinal-cells
#19
Imen Nasri, Rachid Chawech, Cynthia Girardi, Emmanuel Mas, Audrey Ferrand, Nathalie Vergnolle, Nicolas Fabre, Raoudha Mezghani-Jarraya, Claire Racaud-Sultan
CONTEXT AND OBJECTIVE: Diplotaxis harra (Forssk.) Boiss. (Brassicaceae) is traditionally used as an antidiabetic, anti-inflammatory or anticancer agent. In these pathologies, the glycogen synthase kinase 3 β (GSK3β) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3β and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3β. MATERIALS AND METHODS: Methanol extracts from D...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27916091/-tryptase-inhibits-cell-apoptosis-through-upregulating-par-2-and-rho-kinase-in-rheumatoid-arthritis-synovial-fibroblasts
#20
Qianqian Zheng, Shigang Li, Yunli Jia, Wei Liu, Lingling Yu, Xianyong Chen, Jinling Wang
Objective To investigate the regulatory effects of tryptase on protease-activated receptors 2 (PAR-2), Rho signal pathway and apoptosis of MH7A rheumatoid arthritis synovial fibroblasts. Methods In MH7A cells, the expression of PAR-2 was measured by flow cytometry; cell apoptosis was examined by annexin V- FITC/PI staining combined with flow cytometry; the expression of Rho kinase was detected by Pull-down assay and Western botting. Results Tryptase upregulated the expression of PAR-2 in MH7A cells, and suppressed Fas-mediated apoptosis of MH7A cells in a dose-dependent manner...
December 2016: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
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