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Protease activated receptor 2

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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
#1
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/29146750/trpm7-transient-receptor-potential-melastatin-like-7-channel-kinase-controls-calcium-responses-in-arterial-thrombosis-and-stroke-in-mice
#2
Sanjeev K Gotru, Wenchun Chen, Peter Kraft, Isabelle C Becker, Karen Wolf, Simon Stritt, Susanna Zierler, Heike M Hermanns, Deviyani Rao, Anne-Laure Perraud, Carsten Schmitz, René P Zahedi, Peter J Noy, Michael G Tomlinson, Thomas Dandekar, Masayuki Matsushita, Vladimir Chubanov, Thomas Gudermann, Guido Stoll, Bernhard Nieswandt, Attila Braun
OBJECTIVE: TRPM7 (transient receptor potential melastatin-like 7 channel) is a ubiquitously expressed bifunctional protein comprising a transient receptor potential channel segment linked to a cytosolic α-type serine/threonine protein kinase domain. TRPM7 forms a constitutively active Mg(2+) and Ca(2+) permeable channel, which regulates diverse cellular processes in both healthy and diseased conditions, but the physiological role of TRPM7 kinase remains largely unknown. APPROACH AND RESULTS: Here we show that point mutation in TRPM7 kinase domain deleting the kinase activity in mice (Trpm7(R/R) ) causes a marked signaling defect in platelets...
November 16, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/29142404/chalepin-a-compound-from-ruta-angustifolia-l-pers-exhibits-cell-cycle-arrest-at-s-phase-suppresses-nuclear-factor-kappa-b-nf-%C3%AE%C2%BAb-pathway-signal-transducer-and-activation-of-transcription-3-stat3-phosphorylation-and-extrinsic-apoptotic-pathway-in-non-small-cell
#3
Jaime Stella Moses Richardson, Norhaniza Aminudin, Sri Nurestri Abd Malek
Background: Plants have been a major source of inspiration in developing novel drug compounds in the treatment of various diseases that afflict human beings worldwide. Ruta angustifolia L. Pers known locally as Garuda has been conventionally used for various medicinal purposes such as in the treatment of cancer. Objective: A dihydrofuranocoumarin named chalepin, which was isolated from the chloroform extract of the plant, was tested on its ability to inhibit molecular pathways of human lung carcinoma (A549) cells...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29141676/platelets-are-activated-in-anca-associated-vasculitis-via-thrombin-pars-pathway-and-can-activate-the-alternative-complement-pathway
#4
Di Miao, Dan-Yang Li, Min Chen, Ming-Hui Zhao
BACKGROUND: In this study, we investigated the mechanism of platelet activation in patients with antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV), as well as the activation of the alternative complement pathway by platelets in AAV. METHODS: CD62P and platelet-leukocyte aggregates in AAV patients were tested by flow cytometry. Platelets were stimulated by plasma from active AAV patients. The effect of the thrombin-protease-activated receptors (PARs) pathway was evaluated by blocking thrombin or PAR1 antagonists...
November 15, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/29141644/lipopolysaccharide-pretreatment-increases-protease-activated-receptor-2-expression-and-monocyte-chemoattractant-protein-1-secretion-in-vascular-endothelial-cells
#5
Hung-Hsing Chao, Po-Yuan Chen, Wen-Rui Hao, Wei-Ping Chiang, Tzu-Hurng Cheng, Shih-Hurng Loh, Yuk-Man Leung, Ju-Chi Liu, Jin-Jer Chen, Li-Chin Sung
BACKGROUND: This study investigated whether lipopolysaccharide (LPS) increase protease-activated receptor-2 (PAR-2) expression and enhance the association between PAR-2 expression and chemokine production in human vascular endothelial cells (ECs). METHODS: The morphology of ECs was observed through microphotography in cultured human umbilical vein ECs (EA. hy926 cells) treated with various LPS concentrations (0, 0.25, 0.5, 1, and 2 μg/mL) for 24 h, and cell viability was assessed using the MTT assay...
November 15, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/29140280/trpv3-channel-in-keratinocytes-in-scars-with-post-burn-pruritus
#6
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/29138532/ubiquitin-specific-protease-2-modulates-the-lipopolysaccharide-elicited-expression-of-proinflammatory-cytokines-in-macrophage-like-hl-60-cells
#7
Hiroshi Kitamura, Takeshi Ishino, Yoshinori Shimamoto, Jun Okabe, Tomomi Miyamoto, Eiki Takahashi, Ichiro Miyoshi
We investigated the regulatory roles of USP2 in mRNA accumulation of proinflammatory cytokines in macrophage-like cells after stimulation with a toll-like receptor (TLR) 4 ligand, lipopolysaccharide (LPS). Human macrophage-like HL-60 cells, mouse macrophage-like J774.1 cells, and mouse peritoneal macrophages demonstrated negative feedback to USP2 mRNA levels after LPS stimulation, suggesting that USP2 plays a significant role in LPS-stimulated macrophages. USP2 knockdown (KD) by short hairpin RNA in HL-60 cells promoted the accumulation of transcripts for 25 of 104 cytokines after LPS stimulation...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/29118913/protease-activated-receptor-2-in-diabetic-nephropathy-a-double-edged-sword
#8
Maaike Waasdorp, JanWillem Duitman, Sandrine Florquin, Arnold C Spek
Diabetic nephropathy is a major microvascular complication of diabetes mellitus, and the leading cause of end stage renal disease worldwide. The pathogenesis of diabetic nephropathy is complex, making the development of novel treatments that stop or reverse the progression of microalbuminuria into end stage renal disease a challenge. Protease activated receptor (PAR)-2 has recently been shown to aggravate disease progression in diabetic nephropathy based upon which it was suggested that PAR-2 would be a potential target for the treatment of diabetic nephropathy...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/29113347/lunasin-functionally-enhances-ldl-uptake-via-inhibiting-pcsk9-and-enhancing-ldlr-expression-in-vitro-and-in-vivo
#9
Lili Gu, Yue Wang, Yaqiong Xu, Qinghua Tian, Gaoxin Lei, Cheng Zhao, Zhan Gao, Qin Pan, Wenfeng Zhao, Liu Nong, Shuhua Tan
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease which regulates serum low-density lipoprotein cholesterol (LDL-C) levels by promoting the degradation of the hepatic low-density lipoprotein receptor (LDLR), and has become an attractive therapeutic target for cholesterol lowering intervention. Lunasin, a 43-amino acid polypeptide initially isolated from soybean, has been previously proven to possess cholesterol lowering activity. Here we identified the down-regulation of PCSK9 expression by lunasin as one new mechanism that increased cell-surface LDLR level and enhanced LDL uptake in vitro and in vivo...
October 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/29100036/nafamostat-mesilate-a-serine-protease-inhibitor-suppresses-interferon-gamma-induced-up-regulation-of-programmed-cell-death-ligand-1-in-human-cancer-cells
#10
Sadamu Homma, Kazumi Hayashi, Kosaku Yoshida, Yukiko Sagawa, Yuko Kamata, Masaki Ito
Programmed cell death ligand-1 (PD-L1) plays a pivotal role in the suppression of antitumour immunity by binding to programmed cell death-1 (PD-1) on tumouricidal cytotoxic T lymphocytes (CTLs), rendering them inactive. As blockade of PD-1/PD-L1 interaction by the monoclonal antibodies induced effective T cell-mediated antitumour response, suppression of PD-L1 expression in tumour cells by the chemical agent might contribute to treatment against malignant tumours. Nafamostat mesilate (NM), a serine protease inhibitor that is frequently used in the clinic, potently suppressed interferon-gamma (IFN-gamma)-induced up-regulation of PD-L1 in cultured human lung cancer cells (HLC-1) at both the messenger RNA (mRNA) and protein levels...
October 28, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29098568/the-signaling-of-protease-activated-receptor-2-activating-peptide-induced-contraction-in-cat-esophageal-smooth-muscle-cells
#11
Hyun Su Ha, Se Eun Lee, Hyun Seok Lee, Gil Hyung Kim, Chan Jong Yoon, Jong Soo Han, Ji-Yun Lee, Uy Dong Sohn
Protease-activated receptors (PARs) are a family of G protein-coupled receptors with a unique activation mechanism involving proteolytic cleavage of the extracellular N-terminal domain of the receptor. PAR2 has a contractile effect on esophageal smooth muscle. We investigate the signaling pathways of the PAR2-activating peptide (PAR2-AP) induced contraction in cat esophageal smooth muscle cells. The length of freshly isolated smooth muscle cells and permeabilized cells from feline esophagus were measured by scanning micrometry, and by confirming molecular basis via western blot analysis...
November 2, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29089436/protease-mediated-suppression-of-drg-neuron-excitability-by-commensal-bacteria
#12
Jessica L Sessenwein, Corey C Baker, Sabindra Pradhananga, Megan E Maitland, Elaine O Petrof, Emma Allen-Vercoe, Curtis Noordhof, David E Reed, Stephen J Vanner, Alan E Lomax
Peripheral pain signaling reflects a balance of pro and anti-nociceptive influences; the contribution by the gastrointestinal (GI) microbiota to this balance has received little attention. Disorders such as inflammatory bowel disease and irritable bowel syndrome are associated with exaggerated visceral nociceptive actions that may involve altered microbial signaling, particularly given the evidence for bacterial dysbiosis. Thus, we tested whether a community of commensal GI bacteria derived from a healthy human donor (microbial ecosystem therapeutics; MET-1) can affect the excitability of male mouse dorsal root ganglion (DRG) neurons...
October 31, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29079648/regulated-intramembrane-proteolysis-emergent-role-in-cell-signalling-pathways
#13
REVIEW
Aonghus J McCarthy, Caroline Coleman-Vaughan, Justin V McCarthy
Receptor signalling events including those initiated following activation of cytokine and growth factor receptors and the well-characterised death receptors (tumour necrosis factor receptor, type 1, FasR and TRAIL-R1/2) are initiated at the cell surface through the recruitment and formation of intracellular multiprotein signalling complexes that activate divergent signalling pathways. Over the past decade, research studies reveal that many of these receptor-initiated signalling events involve the sequential proteolysis of specific receptors by membrane-bound proteases and the γ-secretase protease complexes...
October 27, 2017: Biochemical Society Transactions
https://www.readbyqxmd.com/read/29074272/melanin-transferred-to-keratinocytes-resides-in-non-degradative-endocytic-compartments
#14
Maria S Correia, Hugo Moreiras, Francisco J C Pereira, Matilde V Neto, Tiago C Festas, Abul K Tarafder, José S Ramalho, Miguel C Seabra, Duarte C Barral
Melanin transfer from melanocytes to keratinocytes and subsequent accumulation in the supra-nuclear region is a critical process in skin pigmentation and protection against ultraviolet radiation. We have previously proposed that the main mode of transfer between melanocytes and keratinocytes is through exo/endocytosis of the melanosome core, termed melanocore. In this study, we developed an in vitro uptake assay using melanocores secreted by melanocytes. We show that the uptake of melanocores, but not melanosomes, by keratinocytes is Protease-activated receptor (PAR)-2-dependent...
October 23, 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29069811/extracellular-sphingomyelinase-activity-impairs-tnf-%C3%AE-induced-endothelial-cell-death-via-adam17-activation-and-tnf-receptor-1-shedding
#15
Anselm Sommer, Marie Düppe, Lena Baumecker, Felix Kordowski, Joscha Büch, Johaiber Fuchslocher Chico, Jürgen Fritsch, Stefan Schütze, Dieter Adam, Maria Sperrhacke, Sucharit Bhakdi, Karina Reiss
ADAM17, a prominent member of the "Disintegrin and Metalloproteinase" (ADAM) family, is an important regulator of endothelial cell proliferation and cell survival. The protease controls vital cellular functions through cleavage of growth factors, cytokines and their receptors including transforming growth factor-alpha (TGF-α), tumor necrosis factor-alpha (TNF-α) and TNF-α receptor 1 (TNFR1). TNF-α is the major inducer of endothelial cell death in cardiovascular diseases. The latter are also characterized by elevated plasma and tissue levels of extracellular sphingomyelinase (SMase)...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/29063596/ca-2-dependent-down-regulation-of-human-histamine-h1-receptors-in-chinese-hamster-ovary-cells
#16
Shigeru Hishinuma, Hiroshi Komazaki, Hayato Tsukamoto, Hirokazu Hatahara, Hiroyuki Fukui, Masaru Shoji
Gq/11 protein-coupled human histamine H1 receptors in Chinese hamster ovary (CHO) cells stimulated with histamine undergo clathrin-dependent endocytosis followed by proteasome/lysosome-mediated down-regulation. In the present study, we evaluated the effects of a sustained increase in intracellular Ca(2+) concentrations induced by a receptor-bypassed stimulation with ionomycin, a Ca(2+) ionophore, on the endocytosis and down-regulation of H1 receptors in CHO cells. All cellular and cell-surface H1 receptors were detected by the binding of [(3) H]mepyramine to intact cells sensitive to the hydrophobic and hydrophilic H1 receptor ligands, mepyramine and pirdonium, respectively...
October 24, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29058826/cathepsin-k-activity-controls-cardiotoxin-induced-skeletal-muscle-repair-in-mice
#17
Shinyu Ogasawara, Xian Wu Cheng, Aiko Inoue, Lina Hu, Limei Piao, Chenglin Yu, Hiroki Goto, Wenhu Xu, Guangxian Zhao, Yanna Lei, Guang Yang, Kaoru Kimura, Hiroyuki Umegaki, Guo-Ping Shi, Masafumi Kuzuya
BACKGROUND: Cathepsin K (CatK) is a widely expressed cysteine protease that has gained attention because of its enzymatic and non-enzymatic functions in signalling. Here, we examined whether CatK-deficiency (CatK(-/-) ) would mitigate injury-related skeletal muscle remodelling and fibrosis in mice, with a special focus on inflammation and muscle cell apoptosis. METHODS: Cardiotoxin (CTX, 20 μM/200 μL) was injected into the left gastrocnemius muscle of male wild-type (CatK(+/+) ) and CatK(-/-) mice, and the mice were processed for morphological and biochemical studies...
October 23, 2017: Journal of Cachexia, Sarcopenia and Muscle
https://www.readbyqxmd.com/read/29053741/the-importance-of-propolis-in-alleviating-the-negative-physiological-effects-of-heat-stress-in-quail-chicks
#18
Gamal M K Mehaisen, Rania M Ibrahim, Adel A Desoky, Hosam M Safaa, Osama A El-Sayed, Ahmed O Abass
Heat stress is one of the most detrimental confrontations in tropical and subtropical regions of the world, causing considerable economic losses in poultry production. Propolis, a resinous product of worker honeybees, possesses several biological activities that could be used to alleviate the deleterious effects of high environmental temperature on poultry production. The current study was aimed at evaluating the effects of propolis supplementation to Japanese quail (Coturnix coturnix japonica) diets on the production performance, intestinal histomorphology, relative physiological and immunological parameters, and selected gene expression under heat stress conditions...
2017: PloS One
https://www.readbyqxmd.com/read/29051069/procyanidins-from-cinnamomi-cortex-promote-proteasome-independent-degradation-of-nuclear-nrf2-through-phosphorylation-of-insulin-like-growth-factor-1-receptor-in-a549%C3%A2-cells
#19
Tomokazu Ohnuma, Kazuya Sakamoto, Asumi Shinoda, Chiaki Takagi, Shoko Ohno, Takahito Nishiyama, Kenichiro Ogura, Akira Hiratsuka
Many lines of evidence demonstrate that transcription factor nuclear factor-E2-related factor 2 (Nrf2) plays essential roles in cancer cell proliferation and resistance to chemotherapy, thereby indicating that suppression of abnormal Nrf2 activation is needed for a new therapeutic approach. Our previous studies reported that procyanidins prepared from Cinnamomi Cortex extract (CCE) have an ability to suppress cytoprotective enzymes and cell proliferation in human cancer cells with activated Nrf2. In the present study, we investigated the mechanism of CCE procyanidin-mediated antagonization of Nrf2...
October 16, 2017: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29047011/comparing-pharmacophore-models-derived-from-crystallography-and-nmr-ensembles
#20
Phani Ghanakota, Heather A Carlson
NMR and X-ray crystallography are the two most widely used methods for determining protein structures. Our previous study examining NMR versus X-Ray sources of protein conformations showed improved performance with NMR structures when used in our Multiple Protein Structures (MPS) method for receptor-based pharmacophores (Damm, Carlson, J Am Chem Soc 129:8225-8235, 2007). However, that work was based on a single test case, HIV-1 protease, because of the rich data available for that system. New data for more systems are available now, which calls for further examination of the effect of different sources of protein conformations...
October 19, 2017: Journal of Computer-aided Molecular Design
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