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Protease activated receptor 2

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https://www.readbyqxmd.com/read/28432785/phosphorylation-of-irhom2-at-the-plasma-membrane-controls-mammalian-tace-dependent-inflammatory-and-growth-factor-signalling
#1
Adam Graham Grieve, Hongmei Xu, Ulrike Künzel, Paul Bambrough, Boris Sieber, Matthew Freeman
Proteolytic cleavage and release from the cell surface of membrane-tethered ligands is an important mechanism of regulating intercellular signalling. TACE is a major shedding protease, responsible for the liberation of the inflammatory cytokine TNFα and ligands of the epidermal growth factor receptor. iRhoms, catalytically inactive members of the rhomboid-like superfamily, have been shown to control the ER-to-Golgi transport and maturation of TACE. Here, we reveal that iRhom2 remains associated with TACE throughout the secretory pathway, and is stabilised at the cell surface by this interaction...
April 22, 2017: ELife
https://www.readbyqxmd.com/read/28428279/interaction-between-tumor-cell-surface-receptor-rage-and-proteinase-3-mediates-prostate-cancer-metastasis-to-bone
#2
Mikhail G Kolonin, Anna Sergeeva, Daniela I Staquicini, Tracey L Smith, Christy A Tarleton, Jeffrey J Molldrem, Richard L Sidman, Serena Marchiò, Renata Pasqualini, Wadih Arap
Human prostate cancer often metastasizes to bone, but the biological basis for such site-specific tropism remains largely unresolved. Recent work led us to hypothesize that this tropism may reflect pathogenic interactions between RAGE, a cell surface receptor expressed on malignant cells in advanced prostate cancer, and proteinase 3 (PR3), a serine protease present in inflammatory neutrophils and hematopoietic cells within the bone marrow microenvironment. In this study, we establish that RAGE-PR3 interaction mediates homing of prostate cancer cells to the bone marrow...
April 20, 2017: Cancer Research
https://www.readbyqxmd.com/read/28426164/protease-activated-receptor-2-suppresses-interleukin-il-10-expression-in-b-cells-via-up-regulating-bcl2l12-in-patients-with-allergic-rhinitis
#3
Jin-Mei Xue, Li-Tao Yang, Gui Yang, Xiao-Rui Geng, Zhi-Qiang Liu, Shuai Wang, Hai-Liang Zhao, Zhi-Gang Liu, Chang-Qing Zhao, Ping-Chang Yang
BACKGROUND AND AIMS: The function of interleukin (IL)-10 producing B cells (B10 cell) is compromised in patients with allergic diseases. Protease-activated receptor (PAR)-2 has immune regulatory functions. This study aims to elucidate the role of PAR2 in the suppression of IL-10 expression in peripheral B cells. METHODS: Peripheral blood B cells were collected from patients with allergic rhinitis (AR). A correlation between the expression of Bcl2 like protein 12 (Bcl2L12) and IL-10 in the B cells was analyzed...
April 20, 2017: Allergy
https://www.readbyqxmd.com/read/28418856/low-density-lipoprotein-receptor-related-protein-6-is-a-novel-coreceptor-of-protease-activated-receptor-2-in-the-dynamics-of-cancer-associated-%C3%AE-catenin-stabilization
#4
Jeetendra Kumar Nag, Arun Kancharla, Myriam Maoz, Hagit Turm, Daniel Agranovich, Chhedi Lal Gupta, Beatrice Uziely, Rachel Bar-Shavit
Protease-activated receptor-2 (PAR2) plays a central role in cancer; however, the molecular machinery of PAR2-instigated tumors remains to be elucidated. We show that PAR2 is a potent inducer of β-catenin stabilization, a core process in cancer biology, leading to its transcriptional activity. Novel association of low-density lipoprotein-related protein 6 (LRP6), a known coreceptor of Frizzleds (Fz), with PAR2 takes place following PAR2 activation. The association between PAR2 and LRP6 was demonstrated employing co-immunoprecipitation, bioluminescence resonance energy transfer (BRET), and confocal microscopy analysis...
March 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28405139/regulation-of-intestinal-permeability-the-role-of-proteases
#5
REVIEW
Hanne Van Spaendonk, Hannah Ceuleers, Leonie Witters, Eveline Patteet, Jurgen Joossens, Koen Augustyns, Anne-Marie Lambeir, Ingrid De Meester, Joris G De Man, Benedicte Y De Winter
The gastrointestinal barrier is - with approximately 400 m(2) - the human body's largest surface separating the external environment from the internal milieu. This barrier serves a dual function: permitting the absorption of nutrients, water and electrolytes on the one hand, while limiting host contact with noxious luminal antigens on the other hand. To maintain this selective barrier, junction protein complexes seal the intercellular space between adjacent epithelial cells and regulate the paracellular transport...
March 28, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28403576/no-pharmacokinetic-drug-drug-interaction-between-prasugrel-and-vorapaxar-following-multiple-dose-administration-in-healthy-volunteers
#6
Matt S Anderson, Teddy Kosoglou, Paul Statkevich, Jing Li, Jennifer Rotonda, Alan G Meehan, David L Cutler
Vorapaxar is a first-in-class antagonist of the protease-activated receptor-1, the primary thrombin receptor on human platelets, which mediates the downstream effects of thrombin in hemostasis and thrombosis. Prasugrel is a platelet inhibitor that acts as a P2Y12 receptor antagonist through an active metabolite, R-138727. This study investigated the interaction of these 2 platelet antagonists when coadministered. This was a randomized, open-label, multiple-dose study in 54 healthy volunteers consisting of a fixed-sequence crossover and a parallel group design...
April 12, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28387563/curcumin-upregulates-antioxidant-defense-lon-protease-and-heat-shock-protein-70-under-hyperglycemic-conditions-in-human-hepatoma-cells
#7
Shivona Gounden, Anil Chuturgoon
Sirtuin 3 (SIRT3) regulates mitochondrial antioxidant (AO) defense and improves mitochondrial disorders. Curcumin protects mitochondria; however, the mechanisms need investigation. We postulated that curcumin increases AO defense under hyperglycemic conditions in HepG2 cells through SIRT3-mediated mechanisms. Cell viability was determined in HepG2 cells cultured with 5 mM glucose, 19.9 mM mannitol, vehicle control, 10 mM glucose, and 30 mM glucose in the absence or presence of curcumin for 24 h. SIRT3, nuclear factor-kappa B (NF-κB), heat-shock protein 70 (Hsp70), and Lon protein expressions were determined using western blot...
April 7, 2017: Journal of Medicinal Food
https://www.readbyqxmd.com/read/28376844/carboxylate-derivatives-of-tributyltin-iv-complexes-as-anticancer-and-antileishmanial-agents
#8
Durdana Waseem, Arshad Farooq Butt, Ihsan-Ul Haq, Moazzam Hussain Bhatti, Gul Majid Khan
BACKGROUND: Tributyltin (IV) compounds are promising candidates for drug development. In the current study, we evaluated in-vitro and in-silico profile of carboxylate derivatives of tributyltin (IV) complexes. METHODS: ADMET and drug-likeliness properties were predicted using MetaPrint2D React, preADMET, SwissADME and Molsoft tools. SwissTargetPrediction predicted molecular targets for compounds. In-vitro bioactivity was evaluated by quantifying cytotoxicity against HepG2, THP-1 cell lines, isolated lymphocytes and leishmania promastigotes as well as measuring protein kinase (PK) inhibition activity...
April 4, 2017: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/28374503/tryptase-potentiates-enteric-nerve-activation-by-histamine-and-serotonin-relevance-for-the-effects-of-mucosal-biopsy-supernatants-from-irritable-bowel-syndrome-patients
#9
D Ostertag, A Annahazi, D Krueger, K Michel, I E Demir, G O Ceyhan, F Zeller, M Schemann
BACKGROUND: We previously showed that mucosal biopsy supernatants from irritable bowel syndrome patients activated neurons despite low concentrations of tryptase, histamine, and serotonin which individually would not cause spike discharge. We studied the potentiating responses between these mediators on excitability of enteric neurons. METHODS: Calcium-imaging was performed using the calcium-sensitive dye Fluo-4 AM in human submucous plexus preparations from 45 individuals...
April 4, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28372987/disrupting-sensitization-of-trpv4
#10
Konrad Mack, Michael J M Fischer
TRPV4 ion channels have a broad expression profile and were shown to contribute to enhanced pain sensation in inflammation. Directly blocking TRPV4 might run the risk of interfering with normal physiology, and has prompted to explore the interaction with the scaffolding protein AKAP79, an approach successfully used for TRPV1 channels. HEK293t cells express AKAP79, additional transfection did not sensitize human TRPV4. Application of trypsin facilitated responses to TRPV4 agonist GSK1016790A. Using a specific protease-activated receptor 2 agonist, involvement of an A-kinase anchoring protein in TRPV4 activation was demonstrated by inhibition with AKAP inhibitor peptide Ht31...
April 1, 2017: Neuroscience
https://www.readbyqxmd.com/read/28370344/conformational-dynamics-of-cathepsin-d-and-binding-to-a-small-molecule-bace1-inhibitor
#11
Christopher R Ellis, Cheng-Chieh Tsai, Fang-Yu Lin, Jana Shen
BACE1 is a major therapeutic target for prevention and treatment of Alzheimer's disease. Developing inhibitors that can selectively target BACE1 in favor of other proteases, especially cathepsin D (CatD), has presented significant challenges. Here, we investigate the conformational dynamics and protonation states of BACE1 and CatD using continuous constant pH molecular dynamics with pH replica-exchange sampling protocol. Despite similar structure, BACE1 and CatD exhibit markedly different active site dynamics...
June 5, 2017: Journal of Computational Chemistry
https://www.readbyqxmd.com/read/28369997/gene-expression-profile-after-knockdown-of-usp18-in-hepg2-2-15-cells
#12
Lin Li, Qing-Song Lei, Ling-Na Kong, Shu-Jun Zhang, Bo Qin
In our previous work, we found that the expression of ubiquitin-specific protease 18 (USP18), also known as UBP43, is associated with the efficiency of interferon alpha (IFN-α) treatment in patients with chronic hepatitis B (CHB). To elucidate the influence of USP18 on hepatitis B virus (HBV) replication and the mechanism of this activity, we silenced USP18 by introducing short hairpin RNA (shRNA) into Hepg2.2.15 cells. To identify the changed genes and pathways in Hepg2.2.15-shRNA-USP18 cells, we performed a microarray gene expression analysis to compare the Hepg2...
March 31, 2017: Journal of Medical Virology
https://www.readbyqxmd.com/read/28363980/a-presynaptic-group-iii-mglur-recruits-g%C3%AE-%C3%AE-snare-interactions-to-inhibit-synaptic-transmission-by-cone-photoreceptors-in-the-vertebrate-retina
#13
Matthew J Van Hook, Norbert Babai, Zack Zurawski, Yun Young Yim, Heidi E Hamm, Wallace B Thoreson
G-protein βγ subunits (Gβγ) interact with presynaptic proteins and regulate neurotransmitter release downstream of Ca(2+) influx. To accomplish their roles in sensory signaling, photoreceptor synapses employ specialized presynaptic proteins that support neurotransmission at active zone structures known as ribbons. While several G-protein coupled receptors (GPCRs) influence synaptic transmission at ribbon synapses of cones and other retinal neurons, it is unknown whether Gβγ contributes to these effects...
March 31, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28360106/ca-2-and-calpain-mediate-capsaicin-induced-ablation-of-axonal-terminals-expressing-transient-receptor-potential-vanilloid-1
#14
Sheng Wang, Sen Wang, Jamila Asgar, John Joseph, Jin Y Ro, Feng Wei, James N Campbell, Man-Kyo Chung
Capsaicin is an ingredient in spicy peppers that produces burning pain by activating transient receptor potential vanilloid 1 (TRPV1), a Ca2+-permeable ion channel in nociceptors. Capsaicin also has been used as an analgesic, and its topical administration is approved for the treatment of certain pain conditions. The mechanisms underlying capsaicin-induced analgesia likely involve reversible ablation of nociceptor terminals. However, the mechanisms underlying these effects are not well understood. To visualize TRPV1-lineage axons, a genetically engineered mouse model was used in which a fluorophore is expressed under TRPV1 promoter...
March 30, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28349651/dermasence-refining-gel-modulates-pathogenetic-factors-of-rosacea-in-vitro
#15
C Borelli, B Becker, S Thude, B Fehrenbacher, D Isermann
BACKGROUND: Over the counter cosmetics sold for local treatment of slight to moderate rosacea often state the claim of actively modulating rosacea pathogenesis. Factors involved in the pathogenesis of this common yet complex skin disorder include kallikrein-related peptidase 5 (KLK5), LL-37, as well as protease-activated receptor 2 (PAR2) and vascular endothelial growth factor (VEGF). OBJECTIVE: The objective was to prove the modulating effect of the cosmetic skin care agent Dermasence Refining Gel (DRG) on factors involved in rosacea pathogenesis...
March 27, 2017: Journal of Cosmetic Dermatology
https://www.readbyqxmd.com/read/28344073/role-of-thrombin-par1-pkc%C3%AE-%C3%AE-axis-in-brain-pericytes-in-thrombin-induced-mmp-9-production-and-blood-brain-barrier-dysfunction-in-vitro
#16
Takashi Machida, Shinya Dohgu, Fuyuko Takata, Junichi Matsumoto, Ikuya Kimura, Mariko Koga, Keiko Nakamoto, Atsushi Yamauchi, Yasufumi Kataoka
Thrombin, an essential component in the coagulation cascade, participates in the pathogenesis of brain diseases, such as ischemic stroke, intracerebral hemorrhage, Alzheimer's disease and Parkinson's disease through blood-brain barrier (BBB) dysfunction. It is thought that the thrombin-matrix metalloproteinase (MMP)-9 axis is an important process in the pathogenesis of neurovascular disease, such as BBB dysfunction. We recently reported that brain pericytes are the most MMP-9-releasing cells in response to thrombin stimulation among the BBB-constituting cells...
March 24, 2017: Neuroscience
https://www.readbyqxmd.com/read/28339772/heterologous-desensitization-of-cardiac-%C3%AE-adrenergic-signal-via-hormone-induced-%C3%AE-ar-arrestin-pde4-complexes
#17
Qian Shi, Minghui Li, Delphine Mika, Qin Fu, Sungjin Kim, Jason Phan, Ao Shen, Gregoire Vandecasteele, Yang K Xiang
Aims: Cardiac β-adrenergic receptor (βAR) signaling is susceptible to heterologous desensitization by different neurohormonal stimuli in clinical conditions associated with heart failure. We aim to examine the underlying mechanism of cross talk between βARs and a set of G-protein coupled receptors (GPCRs) activated by hormones/agonists. Methods and results: Rat ventricular cardiomyocytes were used to determine heterologous phosphorylation of βARs under a series of GPCR agonists...
February 21, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28335793/thrombus-leukocytes-exhibit-more-endothelial-cell-specific-angiogenic-markers-than-peripheral-blood-leukocytes-do-in-acute-coronary-syndrome-patients-suggesting-a-possibility-of-trans-differentiation-a-comprehensive-database-mining-study
#18
Hangfei Fu, Nish Vadalia, Eric R Xue, Candice Johnson, Luqiao Wang, William Y Yang, Claudette Sanchez, Jun Nelson, Qian Chen, Eric T Choi, Jian-Xing Ma, Jun Yu, Hong Wang, Xiaofeng Yang
BACKGROUND: Current angiogenic therapies for cancers and cardiovascular diseases have not yet achieved expected benefits, which reflects the need for improved understanding of angiogenesis. In this study, we focused on solving the problem of whether tissues have different angiogenic potentials (APs) in physiological conditions and how angiogenesis is regulated in various disease conditions. METHODS: In healthy and diseased human and mouse tissues, we profiled the expression of 163 angiogenic genes, including transcription regulators (TRs), growth factors and receptors (GF/Rs), cytokines and chemokines (C/Cs), and proteases and inhibitors (P/Is)...
March 23, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28323866/elevated-fecal-peptidase-d-at-onset-of-colitis-in-galphai2-mice-a-mouse-model-of-ibd
#19
Daniel Bergemalm, Robert Kruse, Maria Sapnara, Jonas Halfvarson, Elisabeth Hultgren Hörnquist
BACKGROUND: The identification of novel fecal biomarkers in inflammatory bowel disease (IBD) is hampered by the complexity of the human fecal proteome. On the other hand, in experimental mouse models there is probably less variation. We investigated the fecal protein content in mice to identify possible biomarkers and pathogenic mechanisms. METHODS: Fecal samples were collected at onset of inflammation in Galphai2-/- mice, a well-described spontaneous model of chronic colitis, and from healthy littermates...
2017: PloS One
https://www.readbyqxmd.com/read/28316004/effect-of-the-fxa-inhibitors-rivaroxaban-and-apixaban-on-platelet-activation-in-patients-with-atrial-fibrillation
#20
B Steppich, F Dobler, L C Brendel, G Hessling, S L Braun, A L Steinsiek, I Deisenhofer, A Hyseni, M Roest, I Ott
Rivaroxaban and Apixaban, increasingly used for stroke prevention in non-valvular atrial fibrillation (AF), might impact platelet reactivity directly or indirectly. By inhibition of Factor Xa (FXa) they preclude not only generation of relevant thrombin amounts but also block signalling of FXa via protease activated receptors. However, weather FXa-inhibition affects platelet haemostasis remains incompletely known. One hundred and twenty-eight patients with AF on chronic anticoagulation with either Rivaroxaban or Apixaban for at least 4 weeks were included in the study...
May 2017: Journal of Thrombosis and Thrombolysis
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