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https://www.readbyqxmd.com/read/28523478/anti-gpvi-fab-sar264565-effectively-blocks-gpvi-function-in-ex-vivo-human-platelets-under-arterial-shear-in-a-perfusion-chamber
#1
Peter Florian, Peter Wonerow, Sebastian Harder, Karina Kuczka, Michel Dubar, Jochen Graff
INTRODUCTION: Glycoprotein VI (GPVI) is the major platelet receptor for collagen-mediated platelet adhesion and activation. SAR264565 is an anti-GPVI-Fab, binds to GPVI with high affinity, and blocks GPVI function in human platelets in vitro. METHODS: The effect of SAR26456 on platelet responsiveness in the blood of 21 healthy male subjects was investigated using Sakariassen's ex vivo thrombogenesis perfusion chamber model on a collagen-coated surface under conditions mimicking arterial flow...
May 18, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28441661/defective-platelet-activation-and-bleeding-complications-upon-cholestasis-in-mice
#2
Nina Sarah Gowert, Meike Klier, Maria Reich, Friedrich Reusswig, Lili Donner, Verena Keitel, Dieter Häussinger, Margitta Elvers
BACKGROUND/AIMS: Platelets are essential mediators of hemostasis to avoid excessive blood loss. Cirrhosis and chronic liver diseases are characterized by alterations in hemostasis. Alterations in the secondary hemostasis have been well studied, while defects in primary hemostasis, especially the consequences of cholestatic liver disease on platelet function are not well defined. METHODS: After bile duct ligation (BDL) platelet activation and thrombus formation were analyzed in mice...
April 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28415757/an-absence-of-platelet-activation-following-thalidomide-treatment-in-vitro-or-in-vivo
#3
Jianlin Qiao, Yulu Wu, Xiaoqing Wu, Yun Liu, Xiaoqian Li, Wen Ju, Kunming Qi, Depeng Li, Elizabeth E Gardiner, Robert K Andrews, Lingyu Zeng, Kailin Xu
Increased risk of thromboembolism and platelet hyperreactivity has been reported in patients receiving thalidomide therapy. Whether thalidomide induces platelet activation directly or through other factors remains unclear. The aim of this study was to evaluate the effect of thalidomide on platelet activation under resting conditions in vitro and in vivo. Isolated human or mouse platelets were treated with different concentrations of thalidomide (10, 50 and 100 μg/ml) for 60 min at 37°C followed by analysis of platelet surface expression of platelet receptors GPIbα, GPVI, αIIbβ3 and P-selectin, and PAC-1 or fibrinogen binding, by flow cytometry and collagen- or ADP-induced platelet aggregation...
March 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28404545/doxepin-inhibits-gpvi-dependent-platelet-ca-2-signaling-and-collagen-dependent-thrombus-formation
#4
Sascha Geue, Britta Walker-Allgaier, Daniela Eißler, Roland Tegtmeyer, Malte Schaub, Florian Lang, Meinrad Gawaz, Oliver Borst, Patrick Münzer
Platelet adhesion, activation and aggregation are essential for primary haemostasis, but are also critically involved in the development of acute arterial thrombotic occlusion. Stimulation of the collagen receptor glyocoprotein VI (GPVI) leads to PLCγ-dependent IP3 production with subsequent platelet activation, due to increased intracellular calcium concentration ([Ca(2+)]i). Although it has been described that tricyclic antidepressants potentially impair platelet activation, nothing is hitherto known about potential effects of the tricyclic antidepressant doxepin on platelet Ca(2+) signaling and thrombus formation...
April 12, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28337278/synthesis-of-huaicarbon-a-b-and-their-activating-effects-on-platelet-glycoprotein-vi-receptor-to-mediate-collagen-induced-platelet-aggregation
#5
Hongli Yu, Yeqing Chen, Hao Wu, Kuilong Wang, Liping Liu, Xingde Zhang
Quercetin and rhamnose were efficiently converted into huaicarbon A/B by heating at 250°C for 10-15 min or at 200°C for 25-30 min. With the optimum molar ratio of quercetin/rhamnose (1:3), huaicarbon A and B yields reached 25% and 16% respectively after heating at 250°C, with 55% quercetin conversion. Huaicarbon A/B both promoted washed platelet aggregation dose-dependently, which was antagonized by an inhibitor of glycoprotein VI (GPVI) receptor. Similarly, they both promoted collagen-induced platelet aggregation in platelet-rich plasma in dose-dependent manners...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28283589/tula-2-protein-phosphatase-suppresses-activation-of-syk-through-the-gpvi-platelet-receptor-for-collagen-by-dephosphorylating-tyr-p-346-a-regulatory-site-of-syk
#6
Kevin Reppschläger, Jeanne Gosselin, Carol A Dangelmaier, Dafydd H Thomas, Nick Carpino, Steven E McKenzie, Satya P Kunapuli, Alexander Y Tsygankov
No abstract text is available yet for this article.
March 10, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28278197/the-role-of-platelet-and-endothelial-garp-in-thrombosis-and-hemostasis
#7
Elien Vermeersch, Frederik Denorme, Wim Maes, Simon F De Meyer, Karen Vanhoorelbeke, Justin Edwards, Ethan M Shevach, Derya Unutmaz, Hodaka Fujii, Hans Deckmyn, Claudia Tersteeg
BACKGROUND: Glycoprotein-A Repetitions Predominant protein (GARP or LRRC32) is present on among others human platelets and endothelial cells. Evidence for its involvement in thrombus formation was suggested by full knockout of GARP in zebrafish. OBJECTIVES: To evaluate the role of GARP in platelet physiology and in thrombus formation using platelet and endothelial conditional GARP knock out mice. METHODS: Platelet and endothelial specific GARP knockout mice were generated using the Cre-loxP recombination system...
2017: PloS One
https://www.readbyqxmd.com/read/28254816/rxr-ligands-negatively-regulate-thrombosis-and-hemostasis
#8
Amanda J Unsworth, Gagan D Flora, Parvathy Sasikumar, Alexander P Bye, Tanya Sage, Neline Kriek, Marilena Crescente, Jonathan M Gibbins
OBJECTIVE: Platelets have been found to express intracellular nuclear receptors including the retinoid X receptors (RXRα and RXRβ). Treatment of platelets with ligands of RXR has been shown to inhibit platelet responses to ADP and thromboxane A2; however, the effects on responses to other platelet agonists and the underlying mechanism have not been fully characterized. APPROACH AND RESULTS: The effect of 9-cis-retinoic acid, docosahexaenoic acid and methoprene acid on collagen receptor (glycoprotein VI [GPVI]) agonists and thrombin-stimulated platelet function; including aggregation, granule secretion, integrin activation, calcium mobilization, integrin αIIbβ3 outside-in signaling and thrombus formation in vitro and in vivo were determined...
May 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/28245414/-advances-of-studies-on-platelet-gpvi-as-antithrombotic-target-review
#9
Pan Li, Jian-Lin Qiao, Kai-Lin Xu
Platelet activation is a crucial step in both physiological hemostasis and pathological thrombosis, which is an important mean to prevent and treat thrombotic diseases by inhibition of platelet activation. The current clinical antithrombotic therapy showed a high efficiency, but at risk of bleeding. Platelet glycoprotein VI (GPVI) is a platelet-specific receptor and its binding with collagen is critical for platelet activation. GPVI antagonists were shown to effectively inhibit thrombosis and inflammation without influence on normal hemostasis...
February 2017: Zhongguo Shi Yan Xue Ye Xue za Zhi
https://www.readbyqxmd.com/read/28164654/expression-of-platelet-collagen-receptor-glycoprotein-vi-in-coronary-heart-disease-interaction-between-platelets-and-endothelial-cells
#10
Jian Shi, Ning Zhu, Jiwen Wang, Yu Wang, Zhaohong Geng, Suya Gao, Zhongyan Li
BACKGROUND: 1) To investigate the expression of platelet collagen receptor glycoprotein VI (GPVI) on the surface of platelets in patients with coronary heart disease (CHD). 2) To investigate the expression of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) on the surface of endothelial cells after exposure to subjects' platelets. METHODS: Platelets were extracted from blood samples of 97 subjects including 43 with acute coronary syndrome (ACS), 21 with stable angina pectoris (SAP), and 33 serving as controls in which CHD was excluded...
July 1, 2016: Clinical Laboratory
https://www.readbyqxmd.com/read/28155721/computer-prediction-of-paratope-on-antithrombotic-antibody-10b12-and-epitope-on-platelet-glycoprotein-vi-via-molecular-dynamics-simulation
#11
Wenping Liu, Guangjian Liu, Huiyun Zhou, Xiang Fang, Ying Fang, Jianhua Wu
BACKGROUND: Interaction between immunoglobulin-like receptor glycoprotein VI (GPVI) and collagen plays a central role in platelet activation and sequent firm adhesion. Of various antithrombotic agents targeting GPVI, antibody 10B12 is of great potential to block the GPVI-collagen interaction, but less is known about 10B12 paratope and GPVI epitope. METHODS: Along the pathway in the computer strategy presented in our previous work, the 10B12/GPVI complex model was constructed through homology modeling and rigid-body docking, and the molecular dynamics (MD) simulation was used to detect the paratope residues on 10B12 and their partners on GPVI...
December 28, 2016: Biomedical Engineering Online
https://www.readbyqxmd.com/read/28102731/microfluidic-whole-blood-testing-of-platelet-response-to-pharmacological-agents
#12
Ruizhi Li, Tilo Grosser, Scott L Diamond
Platelets present a number of intracellular and transmembrane targets subject to pharmacological modulation, either for cardiovascular disease reduction or as an unintended drug response. Microfluidic devices allow human blood to clot on a defined surface under controlled hemodynamic and pharmacological conditions. The potencies of a number of antiplatelet and anticancer drugs have been tested with respect to platelet deposition on collagen under flow. Inhibitors of cyclooxygenase-1 (COX-1) reduce platelet deposition, either when added ex vivo to blood or ingested orally by patients prior to testing...
January 19, 2017: Platelets
https://www.readbyqxmd.com/read/28058806/clustering-of-glycoprotein%C3%A2-vi-gpvi-dimers-upon-adhesion-to-collagen-as-a-mechanism-to-regulate-gpvi-signaling-in-platelets
#13
N S Poulter, A Y Pollitt, D M Owen, E E Gardiner, R K Andrews, H Shimizu, D Ishikawa, D Bihan, R W Farndale, M Moroi, S P Watson, S M Jung
Essentials Dimeric high-affinity collagen receptor glycoprotein VI (GPVI) is present on resting platelets. Spatio-temporal organization of platelet GPVI-dimers was evaluated using advanced microscopy. Upon platelet adhesion to collagenous substrates, GPVI-dimers coalesce to form clusters. Clustering of GPVI-dimers may increase avidity and facilitate platelet activation SUMMARY: Background Platelet glycoprotein VI (GPVI) binding to subendothelial collagen exposed upon blood vessel injury initiates thrombus formation...
March 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28032533/tetraspanin-tspan9-regulates-platelet-collagen-receptor-gpvi-lateral-diffusion-and-activation
#14
Elizabeth J Haining, Alexandra L Matthews, Peter J Noy, Hanna M Romanska, Helen J Harris, Jeremy Pike, Martina Morowski, Rebecca L Gavin, Jing Yang, Pierre-Emmanuel Milhiet, Fedor Berditchevski, Bernhard Nieswandt, Natalie S Poulter, Steve P Watson, Michael G Tomlinson
The tetraspanins are a superfamily of four-transmembrane proteins, which regulate the trafficking, lateral diffusion and clustering of the transmembrane proteins with which they interact. We have previously shown that tetraspanin Tspan9 is expressed on platelets. Here we have characterised gene-trap mice lacking Tspan9. The mice were viable with normal platelet numbers and size. Tspan9-deficient platelets were specifically defective in aggregation and secretion induced by the platelet collagen receptor GPVI, despite normal surface GPVI expression levels...
December 29, 2016: Platelets
https://www.readbyqxmd.com/read/28004756/alteration-of-platelet-gpvi-signaling-in-st-elevation-myocardial-infarction-patients-demonstrated-by-a-combination-of-proteomic-biochemical-and-functional-approaches
#15
Paula Vélez, Raymundo Ocaranza-Sánchez, Diego López-Otero, Lilian Grigorian-Shamagian, Isaac Rosa, Esteban Guitián, José María García-Acuña, José Ramón González-Juanatey, Ángel García
The platelet-specific collagen receptor glycoprotein VI (GPVI) is critical for the formation of arterial thrombosis in vivo. We analyzed GPVI-activated platelets from ST-elevation myocardial infarction (STEMI) patients and matched stable coronary artery disease (SCAD) controls in order to provide novel clues on the degree of involvement of GPVI signaling in the acute event. Firstly, platelets were isolated from systemic venous blood and activated with the GPVI specific agonist CRP (collagen-related peptide)...
December 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27999100/platelet-hyperreactivity-in-diabetes-focus-on-gpvi-signaling-are-useful-drugs-already-available
#16
Jane F Arthur, Karin Jandeleit-Dahm, Robert K Andrews
Adults with diabetes are 2-4 times more likely to suffer from heart disease or ischemic stroke than adults without diabetes, yet standard antiplatelet therapy, which is the cornerstone for primary and secondary prevention of cardiovascular disease, fails in many patients with diabetes. Three independent but often interrelated variables that contribute to platelet hyperreactivity-high blood glucose, oxidative stress, and elevated vascular shear forces-coexist in patients with diabetes, creating a perilous concurrence of risk factors for cardiovascular events...
January 2017: Diabetes
https://www.readbyqxmd.com/read/27996269/novel-glycoprotein-vi-antagonists-as-antithrombotics-synthesis-biological-evaluation-and-molecular-modeling-studies-on-2-3-disubstituted-tetrahydropyrido-3-4-b-indoles
#17
Shome S Bhunia, Ankita Misra, Imran A Khan, Stuti Gaur, Manish Jain, Surendra Singh, Aaruni Saxena, Thomas Hohlfield, Madhu Dikshit, Anil K Saxena
The development of small molecule inhibitors targeting GPVI has promising therapeutic role, as they inhibit arterial thrombosis with limited risk of bleeding. Among the compounds showing in vivo antithrombotic activity, the most active compound 6b (ED50 = 28.36 μmol/kg po in mice) showed improved inhibition for collagen (IC50 = 6.7 μM), CRP-XL (IC50 = 53.5 μM), and convulxin (CVX) (IC50 = 5.7 μM) mediated platelet aggregation as compared to losartan (LOS) (collagen, IC50 = 10.4 μM; CRP-XL, IC50 = 158 μM; CVX, IC50 = 11 μM) than any of its enantiomers S (6c) (collagen, IC50 = 25...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27965959/a-novel-antithrombotic-mechanism-mediated-by-the-receptors-of-the-kallikrein-kinin-and-renin-angiotensin-systems
#18
REVIEW
Alvin H Schmaier
The contact activation (CAS) and kallikrein/kinin (KKS) systems regulate thrombosis risk in two ways. First, the CAS influences contact activation-induced factor XI activation and thrombin formation through the hemostatic cascade. Second, prekallikrein (PK) and bradykinin of the KKS regulate expression of three vessel wall G-protein-coupled receptors, the bradykinin B2 receptor (B2R), angiotensin receptor 2, and Mas to influence prostacyclin formation. The degree of intravascular prostacyclin formation inversely regulates intravascular thrombosis risk...
2016: Frontiers in Medicine
https://www.readbyqxmd.com/read/27924212/combined-administration-of-the-gpvi-fc-fusion-protein-revacept-with-low-dose-thrombolysis-in-the-treatment-of-stroke
#19
Andreas Reimann, Zhongmin Li, Silvia Goebel, Julia Fassbender, Hans-Peter Holthoff, Meinrad Gawaz, Götz Münch, Martin Ungerer
BACKGROUND: Thrombolytic therapy with recombinant tissue plasminogen activator (rtPA) remains the only approved medication for acute ischemic stroke, but incurs significant bleeding risks. Therefore, approaches to combine lower doses of thrombolytic therapy with other effective drugs aim at improving efficacy and reducing bleeding rates. We examined the safety and therapeutic effects of various dosings of rtPA, either alone or combined with glycoprotein VI-Fc fusion protein (GPVI-Fc, Revacept) on experimental stroke in mice...
January 2016: Heart International
https://www.readbyqxmd.com/read/27896950/ppar%C3%AE-agonists-negatively-regulate-%C3%AE-iib%C3%AE-3-integrin-outside-in-signaling-and-platelet-function-through-up-regulation-of-protein-kinase-a-activity
#20
A J Unsworth, N Kriek, A P Bye, K Naran, T Sage, G D Flora, J M Gibbins
Essentials peroxisome proliferator-activated receptor γ (PPARγ) agonists inhibit platelet function. PPARγ agonists negatively regulate outside-in signaling via integrin αIIbβ3. PPARγ agonists disrupt the interaction of Gα13 with integrin β3. This is attributed to an upregulation of protein kinase A activity. SUMMARY: Background Agonists for the peroxisome proliferator-activated receptor (PPARγ) have been shown to have inhibitory effects on platelet activity following stimulation by GPVI and GPCR agonists...
February 2017: Journal of Thrombosis and Haemostasis: JTH
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