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https://www.readbyqxmd.com/read/28088386/trypsin-induces-biphasic-muscle-contraction-and-relaxation-via-transient-receptor-potential-vanilloid-1-and-neurokinin-receptors-1-2-in-porcine-esophageal-body
#1
Bai Xiaopeng, Yoshimasa Tanaka, Eikichi Ihara, Katsuya Hirano, Kayoko Nakano, Mayumi Hirano, Yoshinao Oda, Kazuhiko Nakamura
Duodenal reflux of fluids containing trypsin relates to refractory gastroesophageal reflux disease (GERD). Esophageal peristalsis and clearance are important factors in GERD pathogenesis. However, the function of trypsin in esophageal body contractility is not fully understood. In this study, effects of trypsin on circular smooth muscle (CSM) and longitudinal smooth muscle (LSM) of the porcine esophageal body were examined. Trypsin elicited a concentration dependent biphasic response, a major contraction and a subsequent relaxation only in CSM...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28057878/pseudoautosomal-abnormalities-in-terminal-azfb-c-deletions-are-associated-with-isochromosomes-yp-and-may-lead-to-abnormal-growth-and-neuropsychiatric-function
#2
A Castro, F Rodríguez, M Flórez, P López, B Curotto, D Martínez, A Maturana, M C Lardone, C Palma, V Mericq, M Ebensperger, F Cassorla
STUDY QUESTION: Are copy number variations (CNVs) in the pseudoautosomal regions (PARs) frequent in subjects with Y-chromosome microdeletions and can they lead to abnormal stature and/or neuropsychiatric disorders? SUMMARY ANSWER: Only subjects diagnosed with azoospermia factor (AZF)b+c deletions spanning to the end of the Y chromosome (i.e. terminal deletions) harbor Y isochromosomes and/or cells 45,X that lead to pseudoautosomal gene CNVs, which were associated with abnormal stature and/or neuropsychiatric disorders...
January 5, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28030866/increase-of-mast-cell-nerve-association-and-neuropeptide-receptor-expression-on-mast-cells-in-perennial-allergic-rhinitis
#3
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
#4
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/27994760/par2-modulators-derived-from-gb88
#5
Mei-Kwan Yau, Ligong Liu, Jacky Y Suen, Junxian Lim, Rink-Jan Lohman, Yuhong Jiang, Adam J Cotterell, Grant D Barry, Jeffrey Y W Mak, David A Vesey, Robert C Reid, David P Fairlie
PAR2 antagonists have potential for treating inflammatory, respiratory, gastrointestinal, neurological, and metabolic disorders, but few antagonists are known. Derivatives of GB88 (3) suggest that all four of its components bind at distinct PAR2 sites with the isoxazole, cyclohexylalanine, and isoleucine determining affinity and selectivity, while the C-terminal substituent determines agonist/antagonist function. Here we report structurally similar PAR2 ligands with opposing functions (agonist vs antagonist) upon binding to PAR2...
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27993717/mapping-transmembrane-residues-of-proteinase-activated-receptor-2-par2-that-influence-ligand-modulated-calcium-signaling
#6
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/27981668/activation-of-protease-activated-receptor-2-mediates-cutaneous-vasodilatation-but-not-sweating-roles-of-nitric-oxide-synthase-and-cyclooxygenase
#7
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/27979585/the-differential-expression-of-protease-activated-receptors-contributes-to-functional-differences-between-dark-and-fair-keratinocytes
#8
Meilang Xue, Haiyan Lin, Ruilong Zhao, Hai Po Helena Liang, Christopher Jackson
BACKGROUND: Dark skin has different properties in comparison to fair skin. Melanocytes have been shown to partly contribute to these differences, however, the involvement of keratinocytes from dark or fair skin is not well demonstrated. OBJECTIVES: This study investigated the proliferation and barrier function of dark keratinocytes (DK) and fair keratinocytes (FK), and the role of protease activated receptor (PAR)1 and PAR2. METHODS: DK and FK were isolated from human neonatal foreskins...
December 5, 2016: Journal of Dermatological Science
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
#9
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/27916875/proteinase-activated-receptor-2-is-a-novel-regulator-of-tgf-%C3%AE-signaling-in-pancreatic-cancer
#10
REVIEW
David Witte, Franziska Zeeh, Thomas Gädeken, Frank Gieseler, Bernhard H Rauch, Utz Settmacher, Roland Kaufmann, Hendrik Lehnert, Hendrik Ungefroren
TGF-β has a dual role in tumorigenesis, acting as a tumor suppressor in normal cells and in the early stages of tumor development while promoting carcinogenesis and metastasis in advanced tumor stages. The final outcome of the TGF-β response is determined by cell-autonomous mechanisms and genetic alterations such as genomic instability and somatic mutations, but also by a plethora of external signals derived from the tumor microenvironment, such as cell-to-cell interactions, growth factors and extracellular matrix proteins and proteolytic enzymes...
November 30, 2016: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/27884442/the-induction-of-the-collagen-capsule-synthesis-by-trichinella-spiralis-is-closely-related-to-protease-activated-receptor-2
#11
Mi Kyung Park, Min Kyoung Cho, Shin Ae Kang, Bo Young Kim, Hak Sun Yu
The muscle-stage larvae of the parasite Trichinella spiralis have the ability to survive within host muscle tissue by virtue of the formation a nurse cell-parasite complex, which is surrounded by collagen. The formation of the complex is initiated by excretory-secretory (ES) proteins produced by the parasite. To determine the mechanisms underlying collagen capsule formation, we investigated the expression levels of several types of collagen genes and TGF-βI signaling-related genes (Smad2 and Smad3) in muscle cells...
October 30, 2016: Veterinary Parasitology
https://www.readbyqxmd.com/read/27809303/par2-regulates-regeneration-transdifferentiation-and-death
#12
Ron Piran, Seung-Hee Lee, Pia Kuss, Ergeng Hao, Robbin Newlin, José Luis Millán, Fred Levine
Understanding the mechanisms by which cells sense and respond to injury is central to developing therapies to enhance tissue regeneration. Previously, we showed that pancreatic injury consisting of acinar cell damage+β-cell ablation led to islet cell transdifferentiation. Here, we report that the molecular mechanism for this requires activating protease-activated receptor-2 (PAR2), a G-protein-coupled receptor. PAR2 modulation was sufficient to induce islet cell transdifferentiation in the absence of β-cells...
November 3, 2016: Cell Death & Disease
https://www.readbyqxmd.com/read/27755539/hypersensitivity-induced-by-activation-of-spinal-cord-par2-receptors-is-partially-mediated-by-trpv1-receptors
#13
Petra Mrozkova, Diana Spicarova, Jiri Palecek
Protease-activated receptors 2 (PAR2) and transient receptor potential vanilloid 1 (TRPV1) receptors in the peripheral nerve endings are implicated in the development of increased sensitivity to mechanical and thermal stimuli, especially during inflammatory states. Both PAR2 and TRPV1 receptors are co-expressed in nociceptive dorsal root ganglion (DRG) neurons on their peripheral endings and also on presynaptic endings in the spinal cord dorsal horn. However, the modulation of nociceptive synaptic transmission in the superficial dorsal horn after activation of PAR2 and their functional coupling with TRPV1 is not clear...
2016: PloS One
https://www.readbyqxmd.com/read/27733370/protease-activated-receptors-in-kidney-disease-progression
#14
REVIEW
Oleg Palygin, Daria V Ilatovskaya, Alexander Staruschenko
Protease-activated receptors (PARs) are members of a well-known family of transmembrane G protein-coupled receptors (GPCRs). Four PARs have been identified to date, of which PAR1 and PAR2 are the most abundant receptors, and have been shown to be expressed in the kidney vascular and tubular cells. PAR signaling is mediated by an N-terminus tethered ligand that can be unmasked by serine protease cleavage. The receptors are activated by endogenous serine proteases, such as thrombin (acts on PARs 1, 3, and 4) and trypsin (PAR2)...
December 1, 2016: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/27677841/campylobacter-concisus-pathotypes-induce-distinct-global-responses-in-intestinal-epithelial-cells
#15
Nandan P Deshpande, Marc R Wilkins, Natalia Castaño-Rodríguez, Emily Bainbridge, Nidhi Sodhi, Stephen M Riordan, Hazel M Mitchell, Nadeem O Kaakoush
The epithelial response to the opportunistic pathogen Campylobacter concisus is poorly characterised. Here, we assessed the intestinal epithelial responses to two C. concisus strains with different virulence characteristics in Caco-2 cells using RNAseq, and validated a subset of the response using qPCR arrays. C. concisus strains induced distinct response patterns from intestinal epithelial cells, with the toxigenic strain inducing a significantly more amplified response. A range of cellular functions were significantly regulated in a strain-specific manner, including epithelial-to-mesenchymal transition (NOTCH and Hedgehog), cytoskeletal remodeling, tight junctions, inflammatory responses and autophagy...
September 28, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27615543/deregulated-matriptase-activity-in-oral-squamous-cell-carcinoma-promotes-the-infiltration-of-cancer-associated-fibroblasts-by-paracrine-activation-of-protease-activated-receptor-2
#16
Ai Kanemaru, Koji Yamamoto, Makiko Kawaguchi, Tsuyoshi Fukushima, Chen-Yong Lin, Michael D Johnson, Eric Camerer, Hiroaki Kataoka
Cancer-associated fibroblasts (CAFs) are known to contribute to cancer progression. We have reported that cell surface expression of hepatocyte growth factor activator inhibitor 1 (HAI-1) is decreased in invasive oral squamous cell carcinoma (OSCC) cells. This study examined if HAI-1-insufficiency contributes to CAF recruitment in OSCC. Serum-free conditioned medium (SFCM) from a human OSCC line (SAS) stimulated the migration of 3 human fibroblast cell lines, NB1RGB, MRC5 and KD. SFCM from HAI-1-knockdown SAS showed an additive effect on the migration of NB1RGB and MRC5, but not KD...
January 1, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/27613872/targeting-liver-fibrosis-with-a-cell-penetrating-protease-activated-receptor-2-par2-pepducin
#17
Andrew M Shearer, Rajashree Rana, Karyn Austin, James D Baleja, Nga Nguyen, Andrew Bohm, Lidija Covic, Athan Kuliopulos
Chronic liver inflammation and fibrosis in nonalcoholic steatohepatitis can lead to cirrhosis and liver failure for which there are currently no approved treatments. Protease-activated receptor-2 (PAR2) is an emerging new target expressed on liver stellate cells and hepatocytes that regulates the response to liver injury and inflammation. Here, we identified a pepducin to block the deleterious actions of PAR2 in promoting liver fibrosis. Non-alcoholic fatty liver disease and early fibrosis were induced by the methionine-choline-deficient diet in mice...
October 28, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27604412/allergens-stimulate-store-operated-calcium-entry-and-cytokine-production-in-airway-epithelial-cells
#18
Amit Jairaman, Chelsea H Maguire, Robert P Schleimer, Murali Prakriya
Aberrant immune responses to environmental allergens including insect allergens from house dust mites and cockroaches contribute to allergic inflammatory diseases such as asthma in susceptible individuals. Airway epithelial cells (AECs) play a critical role in this process by sensing the proteolytic activity of allergens via protease-activated receptors (PAR2) to initiate inflammatory and immune responses in the airway. Elevation of cytosolic Ca(2+) is an important signaling event in this process, yet the fundamental mechanism by which allergens induce Ca(2+) elevations in AECs remains poorly understood...
September 8, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27600555/pharmacophore-based-virtual-screening-biological-evaluation-and-binding-mode-analysis-of-a-novel-protease-activated-receptor-2-antagonist
#19
Nam-Chul Cho, Seoung-Hwan Seo, Dohee Kim, Ji-Sun Shin, Jeongmin Ju, Jihye Seong, Seon Hee Seo, Iiyoun Lee, Kyung-Tae Lee, Yun Kyung Kim, Kyoung Tai No, Ae Nim Pae
Protease-activated receptor 2 (PAR2) is a G protein-coupled receptor, mediating inflammation and pain signaling in neurons, thus it is considered to be a potential therapeutic target for inflammatory diseases. In this study, we performed a ligand-based virtual screening of 1.6 million compounds by employing a common-feature pharmacophore model and two-dimensional similarity search to identify a new PAR2 antagonist. The common-feature pharmacophore model was established based on the biological screening results of our in-house library...
August 2016: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/27599717/oligoubiquitination-of-tissue-factor-on-lys255-promotes-ser253-dephosphorylation-and-terminates-tf-release
#20
Camille Ettelaie, Mary E W Collier, Sophie Featherby, John Greenman, Anthony Maraveyas
Restriction of tissue factor (TF) activity at the cell surface and TF release are critical for prevention of excessive coagulation. This study examined the regulation of TF dephosphorylation and its release through ubiquitination. A plasmid containing the sequence to express the tandem protein TF-tGFP was mutated to include an arginine-substitution at Lys255 within TF. MDA-MB-231 cell line, and HCAEC endothelial cells were transfected and subsequently activated with PAR2-agonist peptide. The wild-type and mutant TF-tGFP were immunoprecipitated from the cell lysates and the ubiquitination and phosphorylation state of TF examined...
November 2016: Biochimica et Biophysica Acta
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