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https://www.readbyqxmd.com/read/29345066/protease-activated-receptor-2-is-necessary-for-neutrophil-chemorepulsion-induced-by-trypsin-tryptase-or-dipeptidyl-peptidase-iv
#1
Michael J V White, Luis E Chinea, Darrell Pilling, Richard H Gomer
Compared to neutrophil chemoattractants, relatively little is known about the mechanism neutrophils use to respond to chemorepellents. We previously found that the soluble extracellular protein dipeptidyl peptidase IV (DPPIV) is a neutrophil chemorepellent. In this report, we show that an inhibitor of the protease activated receptor 2 (PAR2) blocks DPPIV-induced human neutrophil chemorepulsion, and that PAR2 agonists such as trypsin, tryptase, 2f-LIGRL, SLIGKV, and AC55541 induce human neutrophil chemorepulsion...
January 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29339138/hyperglycaemia-disrupts-conducted-vasodilation-in-the-resistance-vasculature-of-db-db-mice
#2
Hamish A L Lemmey, Xi Ye, Hong Ding, Chris R Triggle, Christopher J Garland, Kim A Dora
Vascular dysfunction in small resistance arteries is observed during chronic elevations in blood glucose. Hyperglycaemia-associated effects on endothelium-dependent vasodilation have been well characterized, but effects on conducted vasodilation in the resistance vasculature are not known. Small mesenteric arteries were isolated from healthy and diabetic db/db mice, which were used as a model of chronic hyperglycaemia. Endothelium-dependent vasodilation via the Gq/11-coupled proteinase activated receptor 2 (PAR2) was stimulated with the selective agonist SLIGRL...
January 12, 2018: Vascular Pharmacology
https://www.readbyqxmd.com/read/29333924/dynamic-mr-imaging-for-functional-vascularization-depends-on-tissue-factor-signaling-in-glioblastoma
#3
Xiao Chen, Tian Xie, Jingqin Fang, Wei Xue, Houyi Kang, Haipeng Tong, Yu Guo, Bo Zhang, Sumei Wang, Yizeng Yang, Weiguo Zhang
Glomeruloid vascular proliferation (GVP) is a diagnostic hallmark and links to aggressive behavior, therapy resistance and poor prognosis in glioblastoma (GBM). It lacks clinical approaches to predict and monitor its formation and dynamic change. Yet the mechanism of GVPs also remains largely unknown. Using an in situ GBM xenograft mouse model, combined clinical MRI images of pre-surgery tumor and pathological investigation, we demonstrated that the inhibition of tissue factor (TF) decreased GVPs in Mouse GBM xenograft model...
January 15, 2018: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/29317264/the-genetics-of-chronic-itch-gene-expression-in-the-skin-of-atopic-dermatitis-and-psoriasis-patients-with-severe-itch
#4
Leigh A Nattkemper, Hong Liang Tey, Rodrigo Valdes-Rodriguez, Helen Lee, Nicholas K Mollanazar, Christian Albornoz, Kristen M Sanders, Gil Yosipovitch
To identify itch-related mediators and receptors that are differentially expressed in pruritic skin, we used RNA sequencing to analyze the complete transcriptome in skin from paired itchy, lesional and non-itchy, non-lesional skin biopsies from 25 atopic dermatitis (AD) and 25 psoriasis patients and site-matched biopsies from 30 healthy controls. This analysis identified 18,000 differentially expressed genes common between itchy atopic and psoriatic skin compared to healthy skin. Of those, almost 2,000 genes were differentially expressed between itchy and non-itchy skin in atopic and psoriatic subjects...
January 6, 2018: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29316408/agonists-and-antagonists-of-protease-activated-receptor-2-discovered-within-a-dna-encoded-chemical-library-using-mutational-stabilization-of-the-target
#5
Dean G Brown, Giles A Brown, Paolo Centrella, Kaan Certel, Robert M Cooke, John W Cuozzo, Niek Dekker, Christoph E Dumelin, Andrew Ferguson, Cédric Fiez-Vandal, Stefan Geschwindner, Marie-Aude Guié, Sevan Habeshian, Anthony D Keefe, Oliver Schlenker, Eric A Sigel, Arjan Snijder, Holly T Soutter, Linda Sundström, Dawn M Troast, Giselle Wiggins, Jing Zhang, Ying Zhang, Matthew A Clark
The discovery of ligands via affinity-mediated selection of DNA-encoded chemical libraries is driven by the quality and concentration of the protein target. G-protein-coupled receptors (GPCRs) and other membrane-bound targets can be difficult to isolate in their functional state and at high concentrations, and therefore have been challenging for affinity-mediated selection. Here, we report a successful selection campaign against protease-activated receptor 2 (PAR2). Using a thermo-stabilized mutant of PAR2, we conducted affinity selection using our >100-billion-compound DNA-encoded library...
January 1, 2018: SLAS Discovery
https://www.readbyqxmd.com/read/29301867/protease-signaling-regulates-apical-cell-extrusion-cell-contacts-and-proliferation-in-epithelia
#6
Antonino Schepis, Adrian Barker, Yoga Srinivasan, Eaman Balouch, Yaowu Zheng, Ian Lam, Hilary Clay, Chung-Der Hsiao, Shaun R Coughlin
Mechanisms that sense and regulate epithelial morphogenesis, integrity, and homeostasis are incompletely understood. Protease-activated receptor 2 (Par2), the Par2-activating membrane-tethered protease matriptase, and its inhibitor, hepatocyte activator inhibitor 1 (Hai1), are coexpressed in most epithelia and may make up a local signaling system that regulates epithelial behavior. We explored the role of Par2b in matriptase-dependent skin abnormalities in Hai1a-deficient zebrafish embryos. We show an unexpected role for Par2b in regulation of epithelial apical cell extrusion, roles in regulating proliferation that were opposite in distinct but adjacent epithelial monolayers, and roles in regulating cell-cell junctions, mobility, survival, and expression of genes involved in tissue remodeling and inflammation...
January 4, 2018: Journal of Cell Biology
https://www.readbyqxmd.com/read/29289470/prostanoid-dependent-bladder-pain-caused-by-proteinase-activated-receptor-2-activation-in-mice-involvement-of-trpv1-and-t-type-ca2-channels
#7
Maho Tsubota, Tomoka Ozaki, Yuko Hayashi, Yasumasa Okawa, Ayaka Fujimura, Fumiko Sekiguchi, Hiroyuki Nishikawa, Atsufumi Kawabata
We studied the pronociceptive role of proteinase-activated receptor-2 (PAR2) in mouse bladder. In female mice, intravesical infusion of the PAR2-activating peptide, SLIGRL-amide (SL), caused delayed mechanical hypersensitivity in the lower abdomen, namely 'referred hyperalgesia', 6-24 h after the administration. The PAR2-triggered referred hyperalgesia was prevented by indomethacin or a selective TRPV1 blocker, and restored by a T-type Ca2+ channel blocker. In human urothelial T24 cells, SL caused delayed prostaglandin E2 production and COX-2 upregulation...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29261154/the-role-of-par2-in-tgf-%C3%AE-1-induced-erk-activation-and-cell-motility
#8
Hendrik Ungefroren, David Witte, Christian Fiedler, Thomas Gädeken, Roland Kaufmann, Hendrik Lehnert, Frank Gieseler, Bernhard H Rauch
BACKGROUND: Recently, the expression of proteinase-activated receptor 2 (PAR2) has been shown to be essential for activin receptor-like kinase 5 (ALK5)/SMAD-mediated signaling and cell migration by transforming growth factor (TGF)-β1. However, it is not known whether activation of non-SMAD TGF-β signaling (e.g., RAS-RAF-MEK-extracellular signal-regulated kinase (ERK) signaling) is required for cell migration and whether it is also dependent on PAR2. METHODS: RNA interference was used to deplete cells of PAR2, followed by xCELLigence technology to measure cell migration, phospho-immunoblotting to assess ERK1/2 activation, and co-immunoprecipitation to detect a PAR2-ALK5 physical interaction...
December 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29246902/identification-of-the-coagulation-factor-viia-integrin-binding-site-required-for-pro-angiogenic-par2-signaling
#9
Andrea S Rothmeier, Enbo Liu, Sagarika Chakrabarty, Jennifer Disse, Barbara M Mueller, Henrik Østergaard, Wolfram Ruf
The tissue factor (TF) pathway serves both hemostasis and cell signaling, but how cells control these divergent functions of TF remains incompletely understood. TF is the receptor and scaffold of coagulation proteases cleaving protease activated receptor (PAR) 2 that plays pivotal roles in angiogenesis and tumor development. Here we demonstrate that coagulation factor (F) VIIa elicits TF cytoplasmic domain-dependent pro-angiogenic cell signaling independent of the alternative PAR2 activator matriptase. We identify a Lys-Gly-Glu (KGE) integrin binding motif in the FVIIa protease domain that is required for association of the TF-FVIIa complex with the active conformer of integrin β1...
December 15, 2017: Blood
https://www.readbyqxmd.com/read/29246306/factor-vii-induced-microrna-135a-inhibits-autophagy-and-is-associated-with-poor-prognosis-in-hepatocellular-carcinoma
#10
Kuang-Tzu Huang, I-Ying Kuo, Ming-Chao Tsai, Chun-Hsien Wu, Li-Wen Hsu, Li-Yu Chen, Chao-Pin Kung, Yu-Fan Cheng, Shigeru Goto, Yu-Wei Chou, Chao-Long Chen, Chih-Che Lin, Kuang-Den Chen
Hepatocellular carcinoma (HCC) is one of the most common and aggressive malignancies worldwide. Treatment outcomes remain poor mainly due to lack of good diagnostic/prognostic markers and limited therapeutic strategies. We previously characterized aberrant activation of the TF/FVII/PAR2 pathway, which subsequently results in decreased autophagy, as a crucial event in malignant progression of HCC. Here, we identified miR-135a as a highly upregulated miRNA in HCC in response to TF/FVII/PAR2 activation. Analyzing 103 HCC patient specimens, we confirmed that miR-135a was frequently elevated in HCC tissues with higher FVII expression compared to adjacent non-cancerous counterparts...
December 15, 2017: Molecular Therapy. Nucleic Acids
https://www.readbyqxmd.com/read/29230224/lipoarabinomannan-decreases-galectin-9-expression-and-tumor-necrosis-factor-pathway-in-macrophages-favoring-mycobacterium-tuberculosis-intracellular-growth
#11
Leslie Chávez-Galán, Lucero Ramon-Luing, Claudia Carranza, Irene Garcia, Isabel Sada-Ovalle
Lipoarabinomannan (LAM) is a lipid virulent factor secreted by Mycobacterium tuberculosis (Mtb). LAM can be found in the sputum and urine of patients with active tuberculosis. When human monocytes are differentiated into macrophages [monocyte-derived macrophages (MDM)] in the presence of LAM, MDM are poorly functional which may limit the immune response to Mtb infection. Our previous studies have shown that TIM3 and galectin (GAL)9 interaction induces anti-mycobacterial activity, and the expression levels of TIM3 and GAL9 are downregulated during Mtb infection...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29224812/differential-roles-of-kallikrein-related-peptidase-6-in-malignant-transformation-and-%C3%AE-np63%C3%AE-mediated-epithelial-mesenchymal-transition-of-oral-squamous-cell-carcinoma
#12
Naoki Kaneko, Shintaro Kawano, Kaori Yasuda, Yuma Hashiguchi, Taiki Sakamoto, Ryota Matsubara, Yuichi Goto, Teppei Jinno, Yasuyuki Maruse, Masahiko Morioka, Taichi Hattori, Shoichi Tanaka, Hideaki Tanaka, Tamotsu Kiyoshima, Seiji Nakamura
We previously reported that epithelial-to-mesenchymal transition (EMT) was mediated by ΔNp63β in oral squamous cell carcinoma (OSCC). In this study, DNA microarray analyses were performed using ΔNp63β-overexpressing OSCC cells to identify genes associated with ΔNp63β-mediated EMT. Thereby, we focused on kallikrein-related peptidase (KLK) 6, most up-regulated following ΔNp63β-overexpression, that activates protease-activated receptors (PARs). In RT-PCR analyses, ΔNp63 was positively associated with KLK6 and PAR2 and negatively with PAR1 in OSCC cells...
December 2017: Oral Oncology
https://www.readbyqxmd.com/read/29199228/progression-of-time-dependent-changes-to-the-mechanisms-of-vasodilation-by-protease-activated-receptor-2-in-metabolic-syndrome
#13
Kana Maruyama, John J McGuire, Satomi Kagota
Protease-activated receptor 2 (PAR2) is a G protein-coupled receptor activated by serine proteases released from tissues or by synthetic peptide ligands administered pharmacologically. Its wide expression in the cardiovascular system, particularly within the endothelium, vasodilation activity, and link to increased expression of inflammatory cytokines positions PAR2 as a potentially important regulator of vascular pathology under conditions of tissue inflammation, and injury; and thus, a pharmaceutical target for new therapeutics...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29195005/synthetic-indolactam-v-analogs-as-inhibitors-of-par2-induced-calcium-mobilization-in-triple-negative-breast-cancer-cells
#14
Jan Stein, Sonja Stahn, Jörg-Martin Neudörfl, Julia Sperlich, Hans-Günther Schmalz, Nicole Teusch
Human proteinase-activated receptor 2 (PAR2), a transmembrane G-Protein-coupled receptor (GPCR), represents an attractive target for a novel anti-cancer therapy as it plays a critical role in cell migration and invasion. Thus, selective PAR2 inhibitors possess a potential as anti-metastatic drugs. Knowing that the natural product teleocidin A2 is able to inhibit PAR2 in tumor cells, the goal of the present study was to elaborate structure-activity relationships and to identify potent PAR2 inhibitors with lower activity against the adverse target protein kinase C (PKC)...
December 1, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29165389/proteinase-activated-receptor-2-may-drive-cancer-progression-by-facilitating-tgf-%C3%AE-signaling
#15
REVIEW
Hendrik Ungefroren, David Witte, Bernhard H Rauch, Utz Settmacher, Hendrik Lehnert, Frank Gieseler, Roland Kaufmann
The G protein-coupled receptor proteinase-activated receptor 2 (PAR2) has been implicated in various aspects of cellular physiology including inflammation, obesity and cancer. In cancer, it usually acts as a driver of cancer progression in various tumor types by promoting invasion and metastasis in response to activation by serine proteinases. Recently, we discovered another mode through which PAR2 may enhance tumorigenesis: crosstalk with transforming growth factor-β (TGF-β) signaling to promote TGF-β1-induced cell migration/invasion and invasion-associated gene expression in ductal pancreatic adenocarcinoma (PDAC) cells...
November 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29163803/hat1-induces-lung-cancer-cell-apoptosis-via-up-regulating-fas
#16
Na Han, Lei Shi, Qiuyun Guo, Wei Sun, Yang Yu, Li Yang, Xiaoxi Zhang, Mengxian Zhang
The dysfunction of apoptosis is one of the factors contributing to lung cancer (LC) growth. Histone acetyltransferase HAT1 can up regulate cell apoptosis. This study aims to investigate the mechanism by which HAT1 induces LC cell (LCC) apoptosis via up regulating the expression of Fas. In this study, the surgically removed human LC tissues were collected. LCCs were isolated from the LC tissues and analyzed for the expression of HAT1 and Fas by RT-qPCR and Western blotting. We observed that the expression of Fas was negatively correlated with PAR2 in LCCs...
October 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/29148820/a-functional-kinase-short-interfering-ribonucleic-acid-screen-using-protease-activated-receptor-2-dependent-opening-of-transient-receptor-potential-vanilloid-4
#17
William G Darby, Megan S Grace, Kaylene J Simpson, Owen L Woodman, Peter McIntyre
Protease-activated receptor 2 (PAR2) is a proinflammatory G-protein coupled receptor (GPCR) that is activated by inflammatory proteases, and its activation initiates signaling pathways that modulate the nonselective cation channel transient receptor potential vanilloid-4 (TRPV4). PAR2-dependent opening of TRPV4 has been attributed to kinase activation, but the identity of the responsible enzymes is unknown. Deciphering the signaling pathways involved in the PAR2-dependent opening of TRPV4 may yield new targets for pain treatment...
November 17, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29140280/trpv3-channel-in-keratinocytes-in-scars-with-post-burn-pruritus
#18
Chun Wook Park, Hyun Ji Kim, Yong Won Choi, Bo Young Chung, So-Youn Woo, Dong-Keun Song, Hye One Kim
Post-burn pruritus is a common and distressing sequela of burn scars. Empirical antipruritic treatments usually fail to have a satisfactory outcome because of their limited selectivity and possible side effects. Therefore, novel drug targets need to be identified. Here, we aimed to investigate the possible role of protease-activated receptor 2 (PAR2) and transient receptor potential vanniloid 3 (TRPV3), along with the relation of TRPV3 to thymic stromal lymphopoietin (TSLP). Specimens from normal (unscarred) or burn-scarred (with or without pruritus) tissue were obtained from burn patients for this study...
November 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29131007/proteinase-activated-receptor-2-sensitivity-of-amplified-trpa1-activity-in-skeletal-muscle-afferent-nerves-and-exercise-pressor-reflex-in-rats-with-femoral-artery-occlusion
#19
Jihong Xing, Jianhua Li
BACKGROUND/AIMS: Limb ischemia occurs in peripheral artery disease (PAD). Sympathetic nerve activity (SNA) that regulates blood flow directed to the ischemic limb is exaggerated during exercise in this disease, and transient receptor potential channel A1 (TRPA1) in thin-fiber muscle afferents contributes to the amplified sympathetic response. The purpose of the present study was to determine the role of proteinase-activated receptor-2 (PAR2) in regulating abnormal TRPA1 function and the TRPA1-mediated sympathetic component of the exercise pressor reflex...
November 6, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29108655/proteinase-activated-receptor-2-distribution-and-expression-in-equine-small-intestine-tracts-following-herniation-through-the-epiploic-foramen
#20
Noemi Romagnoli, Augusta Zannoni, Chiara Bernardini, Thomas Gobbetti, Cristiano Bombardi, Anna Maria Rambaldi, Maria Morini, Francesco Dondi, Riccardo Rinnovati, Carlotta Lambertini, Alessandro Spadari
Proteinase-activated receptor 2 (PAR2) is a G-protein-coupled receptor for trypsin and mast cell tryptase; it is highly expressed at the intestinal level with multiple functions, such as epithelial permeability and intestinal motility. The aim of the study was to evaluate the distribution and expression of proteinase-activated receptor 2 in the small intestine during herniation through epiploic foramen. In this prospective clinical study, eight horses admitted for colic and which underwent exploratory laparotomy were considered...
October 31, 2017: Research in Veterinary Science
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