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https://www.readbyqxmd.com/read/27933748/exploring-glucocorticoid-receptor-agonists-mechanism-of-action-through-mass-cytometry-and-radial-visualizations
#1
Yann Abraham, Bertran Gerrits, Marie-Gabrielle Ludwig, Michael Rebhan, Caroline Gubser Keller
Recent advances in combining flow cytometry and mass spectrometry have led to the development of mass cytometry, allowing for the interrogation of complex cell populations on an unprecedented scale. The volumes and high dimensionality of mass cytometry data pose significant challenges in terms of analysis and visualization. We implement a method called Radviz (1-3), where multidimensional single cell data can be visualized as a projection that maintains the original dimensions and data complexity whilst facilitating analysis and visualization...
December 9, 2016: Cytometry. Part B, Clinical Cytometry
https://www.readbyqxmd.com/read/27933735/danazol-has-potential-to-cause-pkc-translocation-cell-cycle-dysregulation-and-apoptosis-in-breast-cancer-cells
#2
Suman Jyoti Deka, Ashalata Roy, Vibin Ramakrishnan, Debasis Manna, Vishal Trivedi
Danazol, the established clinical drug has given promising therapeutic results in a series of clinical trials with breast cancer patients. Danazol shares structural similarities with several known PKC agonists and fits well into the C1 domain. Danazol binds to the C1b domain of PKC with Kd of 5.64±1.27 μM. MD simulation studies further support that the PKC-Danazol molecular model is stable and showing minimum distortion to the structure during the simulation period. Immunofluorescence and western-blotting studies indicate that MDAMB-231 cells stimulated with danazol exhibit translocation of PKCα to the plasma membrane...
December 9, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27933336/shp-1-activation-inhibits-vascular-smooth-muscle-cell-proliferation-and-intimal-hyperplasia-in-a-rodent-model-of-insulin-resistance-and-diabetes
#3
Weier Qi, Qian Li, Chong Wee Liew, Christian Rask-Madsen, Samuel M Lockhart, Lars Melholt Rasmussen, Yu Xia, Xuanchun Wang, Mogher Khamaisi, Kevin Croce, George L King
AIMS/HYPOTHESIS: Accelerated migration and proliferation of vascular smooth muscle cells (VSMCs) enhances arterial restenosis after angioplasty in insulin resistance and diabetes. Elevation of Src homology 2-containing protein tyrosine phosphatase 1 (SHP-1) induces apoptosis in the microvasculature. However, the role of SHP-1 in intimal hyperplasia and restenosis has not been clarified in insulin resistance and diabetes. METHODS: We used a femoral artery wire injury mouse model, rodent models with insulin resistance and diabetes, and patients with type 2 diabetes...
December 9, 2016: Diabetologia
https://www.readbyqxmd.com/read/27933319/a-metabolic-widget-adjusts-the-phosphoenolpyruvate-dependent-fructose-influx-in-pseudomonas-putida
#4
Max Chavarría, Ángel Goñi-Moreno, Víctor de Lorenzo, Pablo I Nikel
Fructose uptake in the soil bacterium Pseudomonas putida occurs through a canonical phosphoenolpyruvate (PEP)-dependent sugar transport system (PTS(Fru)). The logic of the genetic circuit that rules its functioning is puzzling: the transcription of the fruBKA operon, encoding all the components of PTS(Fru), can escape the repression exerted by the catabolite repressor/activator protein Cra solely in the presence of intracellular fructose-1-P, an agonist formed only when fructose has been already transported...
November 2016: MSystems
https://www.readbyqxmd.com/read/27933094/the-newer-opioid-agonist-treatment-with-lower-substitutive-opiate-doses-is-associated-with-better-toxicology-outcome-than-the-older-harm-reduction-treatment
#5
Jacopo V Bizzarri, Valentina Casetti, Livia Sanna, Angelo Giovanni Icro Maremmani, Luca Rovai, Silvia Bacciardi, Daria Piacentino, Andreas Conca, Icro Maremmani
BACKGROUND: Charge-free heroin use disorder treatment in Italy follows two main approaches, i.e., harm reduction treatment (HRT) strategy in community low-threshold facilities for drug addiction and opioid agonist treatment (OAT) in high-threshold facilities for opioid addiction, focusing on pharmacological maintenance according to the Dole and Nyswander strategy. We aimed to compare the impact of HRT and OAT on patient outcome, as assessed through negativity for drugs on about 1-year urinalyses...
2016: Annals of General Psychiatry
https://www.readbyqxmd.com/read/27933059/formation-of-neutrophil-extracellular-traps-under-low-oxygen-level
#6
Katja Branitzki-Heinemann, Helene Möllerherm, Lena Völlger, Diab M Husein, Nicole de Buhr, Stefanie Blodkamp, Friederike Reuner, Graham Brogden, Hassan Y Naim, Maren von Köckritz-Blickwede
Since their discovery, neutrophil extracellular traps (NETs) have been characterized as a fundamental host innate immune defense mechanism. Conversely, excessive NET-release may have a variety of detrimental consequences for the host. A fine balance between NET formation and elimination is necessary to sustain a protective effect during an infectious challenge. Our own recently published data revealed that stabilization of hypoxia-inducible factor 1α (HIF-1α) by the iron chelating HIF-1α-agonist desferoxamine or AKB-4924 enhanced the release of phagocyte extracellular traps...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/27932954/neuronal-release-of-cytokine-il-3-triggered-by-mechanosensitive-autostimulation-of-the-p2x7-receptor-is-neuroprotective
#7
Jason C Lim, Wennan Lu, Jonathan M Beckel, Claire H Mitchell
Mechanical strain due to increased pressure or swelling activates inflammatory responses in many neural systems. As cytokines and chemokine messengers lead to both pro-inflammatory and neuroprotective actions, understanding the signaling patterns triggered by mechanical stress may help improve overall outcomes. While cytokine signaling in neural systems is often associated with glial cells like astrocytes and microglia, the contribution of neurons themselves to the cytokine response is underappreciated and has bearing on any balanced response...
2016: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/27932872/randomized-controlled-trials-and-real-world-observational-studies-in-evaluating-cardiovascular-safety-of-inhaled-bronchodilator-therapy-in-copd
#8
Peter Kardos, Sally Worsley, Dave Singh, Miguel Román-Rodríguez, David E Newby, Hana Müllerová
Long-acting muscarinic antagonist (LAMA) or long-acting β2-agonist (LABA) bronchodilators and their combination are recommended for the maintenance treatment of chronic obstructive pulmonary disease (COPD). Although the efficacy of LAMAs and LABAs has been well established through randomized controlled trials (RCTs), questions remain regarding their cardiovascular (CV) safety. Furthermore, while the safety of LAMA and LABA monotherapy has been extensively studied, data are lacking for LAMA/LABA combination therapy, and the majority of the studies that have reported on the CV safety of LAMA/LABA combination therapy were not specifically designed to assess this...
2016: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/27932572/a-mechanism-for-acetylcholine-receptor-gating-based-on-structure-coupling-phi-and-flip
#9
Shaweta Gupta, Srirupa Chakraborty, Ridhima Vij, Anthony Auerbach
Nicotinic acetylcholine receptors are allosteric proteins that generate membrane currents by isomerizing ("gating") between resting and active conformations under the influence of neurotransmitters. Here, to explore the mechanisms that link the transmitter-binding sites (TBSs) with the distant gate, we use mutant cycle analyses to measure coupling between residue pairs, phi value analyses to sequence domain rearrangements, and current simulations to reproduce a microsecond shut component ("flip") apparent in single-channel recordings...
December 8, 2016: Journal of General Physiology
https://www.readbyqxmd.com/read/27932528/comorbidities-treatment-patterns-and-cost-of-illness-of-acromegaly-in-sweden-a-register-linkage-population-based-study
#10
Eva Lesén, Daniel Granfeldt, Aude Houchard, Jérôme Dinet, Anthony Berthon, Daniel S Olsson, Ingela Björholt, Gudmundur Johannsson
OBJECTIVE: Acromegaly is a complex endocrine disease with multiple comorbidities. Treatment to obtain biochemical remission includes surgery, medical therapy and radiation. We aimed to describe comorbidities, treatment patterns and cost-of-illness in patients with acromegaly in Sweden. DESIGN: A nationwide population-based study. METHODS: Patients with acromegaly were identified and followed in national registers in Sweden. Longitudinal treatment patterns were assessed in patients diagnosed between July 2005 and December 2013...
February 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/27932310/loss-of-dopamine-d1-receptors-and-diminished-d1-5-receptor-mediated-erk-phosphorylation-in-the-periaqueductal-gray-after-spinal-cord-lesion
#11
Pamela J Voulalas, Yadong Ji, Li Jiang, Jamila Asgar, Jin Y Ro, Radi Masri
Neuropathic pain resulting from spinal cord injury is often accompanied by maladaptive plasticity of the central nervous system, including the opioid receptor-rich periaqueductal gray (PAG). Evidence suggests that sensory signaling via the PAG is robustly modulated by dopamine D1- and D2-like receptors, but the effect of damage to the spinal cord on D1 and D2 receptor protein expression and function in the PAG has not been examined. Here we show that 21 days after a T10 or C6 spinothalamic tract lesion, both mice and rats display a remarkable decline in the expression of D1 receptors in the PAG, revealed by western blot analysis...
December 5, 2016: Neuroscience
https://www.readbyqxmd.com/read/27932249/toxicologic-effects-of-28-day-dietary-exposure-to-the-flame-retardant-1-2-dibromo-4-1-2-dibromoethyl-cyclohexane-tbech-in-fischer-rats
#12
Ivan H A Curran, Virginia Liston, Andrée Nunnikhoven, Don Caldwell, Matthew J S Scuby, Peter Pantazopoulos, Dorothea F K Rawn, Laurie Coady, Cheryl Armstrong, David E Lefebvre, Genevieve S Bondy
The brominated flame retardant TBECH is used as an additive to delay ignition and inhibit fires in construction materials and consumer goods. Trends in human exposure are not clear, although humans may be exposed to TBECH via indoor dust and air. In birds and fish there is some evidence of disruption in endocrine and reproductive parameters due to TBECH. In vitro studies indicate that TBECH is an androgen receptor agonist. In this study rats were exposed to 0, 10, 50, 250, 1250 or 5000mg/kg technical TBECH for 28days in diet, corresponding to 0, 0...
December 5, 2016: Toxicology
https://www.readbyqxmd.com/read/27931650/effect-of-non-adrenergic-vasopressors-on-macro-and-microvascular-coupling-in-distributive-shock
#13
REVIEW
M Hessler, T G Kampmeier, S Rehberg
The present review initially describes the rationale for the use of non-adrenergic vasopressors in the treatment of distributive shock and then provides an overview of the individual vasopressin-receptor agonists, namely arginine vasopressin, terlipressin, and selepressin. Following a brief summary of their current use in clinical practice, the present review focuses on the influence of vasopressin-receptor agonists on macro- and microvascular coupling, also referred to as hemodynamic coherence. On the basis of the current evidence from experimental and clinical studies, vasopressin-receptor agonists do not negatively influence macro- and microvascular coupling as compared to the standard therapy with norepinephrine, when used in established treatment regimes...
December 2016: Best Practice & Research. Clinical Anaesthesiology
https://www.readbyqxmd.com/read/27931302/new-insights-into-treatment-of-children-with-exercise-induced-asthma-symptoms
#14
Iwona Stelmach, Anna Sztafiska, Joanna Jerzyska, Daniela Podlecka, Pawe Majak, Wodzimierz Stelmach
BACKGROUND: Exercise is one of the most common triggers of bronchoconstriction and affects up to 80% of children with asthma. OBJECTIVE: The purpose of this randomized, double-blind, placebo-controlled study was to assess the effectiveness of treatment with ciclesonide 160 microgram, either alone, with a higher dose, with a leukotriene receptor antagonist (LTRA), or with a long-acting beta-agonist (LABA) in children with asthma with postexercise-induced symptoms...
November 2016: Allergy and Asthma Proceedings:
https://www.readbyqxmd.com/read/27931288/therapeutic-injection-of-a-c-type-cpg-odn-induced-an-antitumor-immune-response-in-c57-bl6-mice-of-orthotopically-transplanted-hepatocellular-carcinoma
#15
Huijie Jia, Tiesuo Zhao, Di Zou, Xiaolong Jia, Ji Gao, Xiangfeng Song
Synthetic CpG oligodeoxynucleotides (ODNs), as TLR9 agonists, have been found to play a possible role in antitumor effect. In order to determine the effect of YW002, known as a C-type CpG ODN, on the treatment of hepatocellular carcinoma (HCC), which is one of the most aggressive carcinomas, we chose to inject YW002 at the doses of 12.5 g and 25 g per mouse 7 days post-tumor challenge. The survival rate of mice was recorded every day. On day 14 postinjection, five mice in each group were bled and randomly sacrificed...
May 2016: Oncology Research
https://www.readbyqxmd.com/read/27931253/alcohol-use-in-opioid-agonist-treatment
#16
REVIEW
Seonaid Nolan, Jan Klimas, Evan Wood
Alcohol misuse among individuals receiving agonist treatment for an opioid use disorder is common and is associated with significant morbidity and mortality. At present, though substantial research highlights effective strategies for the screening, diagnosis and management of an alcohol or opioid use disorder individually, less is known about how best to care for those with a dual diagnosis especially since common treatments for opioid addiction may be contraindicated in a setting of alcohol use. This review summarizes existing research and characterizes the prevalence, clinical implications and management of alcohol misuse among individuals with opioid addiction...
December 8, 2016: Addiction Science & Clinical Practice
https://www.readbyqxmd.com/read/27931246/increased-alternate-splicing-of-htr2c-in-a-mouse-model-for-prader-willi-syndrome-leads-disruption-of-5ht2c-receptor-mediated-appetite
#17
Alastair S Garfield, Jennifer R Davies, Luke K Burke, Hannah V Furby, Lawrence S Wilkinson, Lora K Heisler, Anthony R Isles
Alternate splicing of serotonin (5-hydroxytryptamine; 5-HT) 2C receptor (5-HT2CR) pre-RNA is negatively regulated by the small nucleolar RNA, Snord115, loss of which is observed in nearly all individuals with Prader-Willi Syndrome (PWS), a multigenic disorder characterised by hyperphagia and obesity. Given the role of the 5-HT2CR in the regulation of ingestive behaviour we investigated the pathophysiological implications of Snord115 deficiency on 5-HT2CR regulated appetite in a genotypically relevant PWS mouse model (PWS-IC)...
December 8, 2016: Molecular Brain
https://www.readbyqxmd.com/read/27931146/d-cycloserine-restores-experience-dependent-neuroplasticity-after-tbi-in-the-developing-rat-brain
#18
Naomi Sulit Sta Maria, Maxine Lane Reger, Yan Cai, Mary Anne Tezheart Mercado Baquing, Floyd Buen, Aditya Ponnaluri, David Hovda, Neil G Harris, Christopher C Giza
Traumatic brain injury (TBI) in children can cause persisting cognitive and behavioral dysfunction and inevitably raises concerns about lost potential in these injured youths. Lateral fluid percussion injury (FPI) in weanling rats pathologically affects hippocampal NMDAR- and AMPAR-mediated glutamatergic neurotransmission subacutely, within the first post-injury week. FPI to weanling rats has also been shown to impair enriched-environment (EE) induced enhancement of Morris water maze (MWM) learning and memory in adulthood...
December 8, 2016: Journal of Neurotrauma
https://www.readbyqxmd.com/read/27930988/potential-involvement-of-ppar-%C3%AE-activation-in-diminishing-the-hepatoprotective-effect-of-fenofibrate-in-nafld-accuracy-of-non-invasive-panel-in-determining-the-stage-of-liver-fibrosis-in-rats
#19
Asmaa M Hamed, Omnyah A El-Kharashi, Suzi S A Boctor, Lobna F Abd-Elaziz
BACKGROUND: Although Fenofibrate (FF) is a hypolipedmic drug and one of the PPARα agonists which is a drug target for non alcoholic liver disease (NAFLD), no studies had investigated its potential hepatic effects in such cases. AIM: To compare between the effect of FF and Gemfibrozil (GF) on the prognosis of NAFLD in rats. METHODS: Sixty four rats were used and classified into two main groups. Group I (treated for 6 weeks): naïve, FF, GF groups and Group II (treated for 14 weeks and drugs were added at the last 6 weeks): Control, high fat diet (HFD) untreated, HFD+FF, HFD+FF+folic acid (FA) and HFD+GF groups...
December 5, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27930985/c1q-tnf-related-protein-3-exerts-the-chondroprotective-effects-in-il-1%C3%AE-treated-sw1353-cells-by-regulating-the-fgfr1-signaling
#20
Yuanxia Huang, Guang Wan, Jingang Tao
Cartilage degeneration is known as a major cause of osteoarthritis (OA). C1q/TNF-related protein-3 (CTRP3) is an adipokine relative to chondrogenesis in vitro. However, its effect on cartilage degeneration in OA remains unclearly. In the present study, SW1353 cells were treated with IL-1β to imitate the microenvironment of OA for vitro research. Then, an obvious down-regulation of CTRP3 were validated in IL-1β-treated SW1353 cells. In addition, CTRP3 overexpression significantly attenuated the decrease in cell proliferation and increase in cell apoptosis triggered by IL-1β...
December 5, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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