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https://www.readbyqxmd.com/read/27936270/the-relative-contribution-of-noise-and-adaptation-to-competition-during-tri-stable-motion-perception
#1
Andrew Isaac Meso, James Rankin, Olivier Faugeras, Pierre Kornprobst, Guillaume S Masson
Animals exploit antagonistic interactions for sensory processing and these can cause oscillations between competing states. Ambiguous sensory inputs yield such perceptual multistability. Despite numerous empirical studies using binocular rivalry or plaid pattern motion, the driving mechanisms behind the spontaneous transitions between alternatives remain unclear. In the current work, we used a tristable barber pole motion stimulus combining empirical and modeling approaches to elucidate the contributions of noise and adaptation to underlying competition...
December 1, 2016: Journal of Vision
https://www.readbyqxmd.com/read/27936102/am251-suppresses-epithelial-mesenchymal-transition-of-renal-tubular-epithelial-cells
#2
Tomoyo Yoshinaga, Kenichiro Uwabe, Shoichi Naito, Kenichi Higashino, Toru Nakano, Yoshito Numata, Akio Kihara
Epithelial-mesenchymal transition (EMT) of renal tubular epithelial cells is one of the causative mechanisms of kidney fibrosis. In our study, we screened lipophilic compounds using a lipid library including approximately 200 lipids to identify those that suppressed EMT induced by a transforming growth factor (TGF)-β1 stimulus. Initial screening was performed with the immortalized HK-2 renal tubule epithelial cell line. The most promising compounds were further tested in RPTEC primary renal tubule epithelial cells...
2016: PloS One
https://www.readbyqxmd.com/read/27935987/patient-reported-treatment-satisfaction-with-rivaroxaban-for-stroke-prevention-in-atrial-fibrillation-a-french-observational-study-the-safari-study
#3
Olivier Hanon, Edouard Chaussade, Pierre Gueranger, Elise Gruson, Sabrina Bonan, Alain Gay
BACKGROUND: For antithrombotic treatments, Patient Reported Outcomes (PRO) and patient satisfaction with treatment are essential data for physicians because of the strong relationship between patient satisfaction and adherence to treatment. The impact of rivaroxaban on patient satisfaction and quality of life was not sufficiently documented in phase III studies. There is a need for further data in this field especially in real life conditions. METHODS: The SAFARI study is composed of patients with non-valvular atrial fibrillation (AF), previously treated with vitamin K antagonist (VKA) and switched to rivaroxaban...
2016: PloS One
https://www.readbyqxmd.com/read/27935941/objectives-and-design-of-bleeds-a-cohort-study-to-identify-new-risk-factors-and-predictors-for-major-bleeding-during-treatment-with-vitamin-k-antagonists
#4
Nienke van Rein, Willem M Lijfering, Mettine H A Bos, Martien H Herruer, Helga W Vermaas, Felix J M van der Meer, Pieter H Reitsma
BACKGROUND: Risk scores for patients who are at high risk for major bleeding complications during treatment with vitamin K antagonists (VKAs) do not perform that well. BLEEDS was initiated to search for new biomarkers that predict bleeding in these patients. OBJECTIVES: To describe the outline and objectives of BLEEDS and to examine whether the study population is generalizable to other VKA treated populations. METHODS: A cohort was created consisting of all patients starting VKA treatment at three Dutch anticoagulation clinics between January-2012 and July-2014...
2016: PloS One
https://www.readbyqxmd.com/read/27935900/-thromboangiitis-obliterans-buerger-s-disease-state-of-the-art
#5
D D Zerbino, E A Zimba, N N Bagry
Thromboangiitis obliterans (Buerger's disease) is systemic vasculitis with predominant development of thrombotic occlusions of small-to-medium diameter arteries of distal portions of both upper and lower limbs. A distinctive feature of Buerger's disease from other vasculitides is the involvement of the venous bed into the pathological process in the form of migrating thrombophlebitis. The disease is encountered more often in young adult males, predominantly tobacco smokers. The clinical pattern is presented by symptoms of increasing insufficiency of blood supply of tissues of extremities...
2016: Angiologii︠a︡ i Sosudistai︠a︡ Khirurgii︠a︡, Angiology and Vascular Surgery
https://www.readbyqxmd.com/read/27935867/the-bromodomain-inhibitor-otx015-mk-8628-exerts-anti-tumor-activity-in-triple-negative-breast-cancer-models-as-single-agent-and-in-combination-with-everolimus
#6
Ramiro Vázquez, María E Riveiro, Lucile Astorgues-Xerri, Elodie Odore, Keyvan Rezai, Eugenio Erba, Nicolò Panini, Andrea Rinaldi, Ivo Kwee, Luca Beltrame, Mohamed Bekradda, Esteban Cvitkovic, Francesco Bertoni, Roberta Frapolli, Maurizio D'Incalci
Triple-negative breast cancer (TNBC) is an aggressive and heterogeneous subgroup of breast tumors clinically defined by the lack of estrogen, progesterone and HER2 receptors, limiting the use of the targeted therapies employed in other breast malignancies. Recent evidence indicates that c-MYC is a key driver of TNBC. The BET-bromodomain inhibitor OTX015 (MK-8628) has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models...
December 7, 2016: Oncotarget
https://www.readbyqxmd.com/read/27935820/s113r-mutation-in-slc33a1-leads-to-neurodegeneration-and-augmented-bmp-signaling-in-a-mouse-model
#7
Pingting Liu, Baichun Jiang, Jian Ma, Pengfei Lin, Yinshuai Zhang, Changshun Shao, Wenjie Sun, Yaoqin Gong
The S113R mutation (c.339T>G) (MIM #603690.0001) in SLC33A1 (MIM #603690), an ER membrane acetyl-CoA transporter, has been previously identified in patients with hereditary spastic paraplegia type 42 (SPG42; MIM #612539). SLC33A1 has also been shown to inhibit bone morphogenetic protein (BMP) signaling pathway in zebrafish. To better understand the function of SLC33A1, we generated and characterized Slc33a1(S113R) knock-in mice. Homozygous Slc33a1(S113R) mutant mice were embryonic lethal, while heterozygous Slc33a1 mutant mice (Slc33a1(wt/mut)) exhibited behavioral abnormalities and central neurodegeneration, which is consistent with HSP phenotypes...
November 24, 2016: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/27935479/structural-basis-for-subtype-specific-inhibition-of-the-p2x7-receptor
#8
Akira Karasawa, Toshimitsu Kawate
The P2X7 receptor is a non-selective cation channel activated by extracellular adenosine triphosphate (ATP). Chronic activation of P2X7 underlies many health problems such as pathologic pain, yet we lack effective antagonists due to poorly understood mechanisms of inhibition. Here we present crystal structures of a mammalian P2X7 receptor complexed with five structurally-unrelated antagonists. Unexpectedly, these drugs all bind to an allosteric site distinct from the ATP-binding pocket in a groove formed between two neighboring subunits...
December 9, 2016: ELife
https://www.readbyqxmd.com/read/27935411/climacteric-ripening-of-apple-fruit-is-regulated-by-transcriptional-circuits-stimulated-by-cross-talks-between-ethylene-and-auxin
#9
Nicola Busatto, Alice Tadiello, Livio Trainotti, Fabrizio Costa
Apple is a fleshy fruit distinguished by a climacteric type of ripening, since most of the relevant physiological changes are triggered and governed by the action of ethylene. After its production, this hormone is perceived by a series of receptors to regulate, through a signaling cascade, downstream ethylene related genes. The possibility to control the effect of ethylene opened new horizons to the improvement of the postharvest fruit quality. To this end, 1-methylcyclopropene (1-MCP), an ethylene antagonist, is routinely used to modulate the ripening progression increasing storage life...
December 9, 2016: Plant Signaling & Behavior
https://www.readbyqxmd.com/read/27935256/pigment-translocation-in-caridean-shrimp-chromatophores-receptor-type-signal-transduction-second-messengers-and-cross-talk-among-multiple-signaling-cascades
#10
Sarah Ribeiro Milograna, Márcia Regina Ribeiro, Fernanda Tinti Bell, John Campbell McNAMARA
Pigment aggregation in shrimp chromatophores is triggered by red pigment concentrating hormone (RPCH), a neurosecretory peptide whose plasma membrane receptor may be a G-protein coupled receptor (GPCR). While RPCH binding activates the Ca(2+) /cGMP signaling cascades, a role for cyclic AMP (cAMP) in pigment aggregation is obscure, as are the steps governing Ca(2+) release from the smooth endoplasmic reticulum (SER). A role for the antagonistic neuropeptide, pigment dispersing homone (α-PDH) is also unclear...
December 9, 2016: Journal of Experimental Zoology. Part A, Ecological Genetics and Physiology
https://www.readbyqxmd.com/read/27935243/mocdc14-is-important-for-septation-during-conidiation-and-appressorium-formation-in-magnaporthe-oryzae
#11
Chaohui Li, Shulin Cao, Chengkang Zhang, Yonghui Zhang, Qiang Zhang, Jin-Rong Xu, Chenfang Wang
As a typical foliar pathogen, appressorium formation and penetration are critical steps in the infection cycle of Magnaporthe oryzae. Because appressorium formation and penetration are closely co-regulated with cell cycle and Cdc14 phosphatases have antagonistic relationship with CDKs on proteins related to mitotic exits and cytokinesis, in this study we functionally characterized the MoCDC14 gene in M. oryzae. The Mocdc14 deletion mutant was significantly reduced in growth rate and conidiation. It also was defective in septum formation and nuclear distribution...
December 9, 2016: Molecular Plant Pathology
https://www.readbyqxmd.com/read/27935083/endometrial-cancer-risk-prediction-including-serum-based-biomarkers-results-from-the-epic-cohort
#12
Renée T Fortner, Anika Hüsing, Tilman Kühn, Meric Konar, Kim Overvad, Anne Tjønneland, Louise Hansen, Marie-Christine Boutron-Ruault, Gianluca Severi, Agnès Fournier, Heiner Boeing, Antonia Trichopoulou, Vasiliki Benetou, Philippos Orfanos, Giovanna Masala, Claudia Agnoli, Amalia Mattiello, Rosario Tumino, Carlotta Sacerdote, H B As Bueno-de-Mesquita, Petra H M Peeters, Elisabete Weiderpass, Inger T Gram, Oxana Gavrilyuk, J Ramón Quirós, José Maria Huerta, Eva Ardanaz, Nerea Larrañaga, Leila Lujan-Barroso, Emilio Sánchez-Cantalejo, Salma Tunå Butt, Signe Borgquist, Annika Idahl, Eva Lundin, Kay-Tee Khaw, Naomi E Allen, Sabina Rinaldi, Laure Dossus, Marc Gunter, Melissa A Merritt, Ioanna Tzoulaki, Elio Riboli, Rudolf Kaaks
Endometrial cancer risk prediction models including lifestyle, anthropometric, and reproductive factors have limited discrimination. Adding biomarker data to these models may improve predictive capacity; to our knowledge, this has not been investigated for endometrial cancer. Using a nested case-control study within the European Prospective Investigation into Cancer and Nutrition (EPIC) cohort, we investigated the improvement in discrimination gained by adding serum biomarker concentrations to risk estimates derived from an existing risk prediction model based on epidemiologic factors...
December 9, 2016: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/27934887/aldosterone-induces-rapid-sodium-intake-by-a-nongenomic-mechanism-in-the-nucleus-tractus-solitarius
#13
Hu Qiao, Bo Hu, Hong Zhou, Jianqun Yan, Ru Jia, Bo Lu, Bo Sun, Xiao Luo, Yuanyuan Fan, Nan Wang
The purpose of this study was to determine whether aldosterone has a rapid action in the nucleus tractus solitarius (NTS) that increases sodium intake, and to examine whether this effect of aldosterone, if present, is mediated by G protein-coupled estrogen receptor (GPER). Adult male Sprague-Dawley rats with a stainless-steel cannula in the NTS were used. Aldosterone was injected into the NTS at the doses of 1, 5, 10 and 20 ng 0.1 μl(-1). A rapid dose-related increase of 0.3 M NaCl intake was induced within 30 min and this increase was not suppressed by the mineralocorticoid receptor (MR) antagonist spironolactone (10 ng 0...
December 9, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27934856/bulk-cell-density-and-wnt-tgfbeta-signalling-regulate-mesendodermal-patterning-of-human-pluripotent-stem-cells
#14
Henning Kempf, Ruth Olmer, Alexandra Haase, Annika Franke, Emiliano Bolesani, Kristin Schwanke, Diana Robles-Diaz, Michelle Coffee, Gudrun Göhring, Gerald Dräger, Oliver Pötz, Thomas Joos, Erik Martinez-Hackert, Axel Haverich, Falk F R Buettner, Ulrich Martin, Robert Zweigerdt
In vitro differentiation of human pluripotent stem cells (hPSCs) recapitulates early aspects of human embryogenesis, but the underlying processes are poorly understood and controlled. Here we show that modulating the bulk cell density (BCD: cell number per culture volume) deterministically alters anteroposterior patterning of primitive streak (PS)-like priming. The BCD in conjunction with the chemical WNT pathway activator CHIR99021 results in distinct paracrine microenvironments codifying hPSCs towards definitive endoderm, precardiac or presomitic mesoderm within the first 24 h of differentiation, respectively...
December 9, 2016: Nature Communications
https://www.readbyqxmd.com/read/27934457/stereoselective-synthesis-of-a-dipyridyl-transient-receptor-potential-vanilloid-3-trpv3-antagonist
#15
Eric A Voight, Jerome F Daanen, Robert G Schmidt, Arthur Gomtsyan, Michael J Dart, Philip R Kym
An efficient asymmetric synthesis of dipyridyl TRPV3 antagonist 1 is reported. The four-step route involves two C-C bond-forming steps, a highly diastereoselective alkene hydration, and asymmetric ketone hydrosilylation in 97% ee.
December 2, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27934233/modeling-membrane-protein-ligand-binding-interactions-the-human-purinergic-platelet-receptor
#16
D'Artagnan Greene, Wesley M Botello-Smith, Alec Follmer, Li Xiao, Eleftherios Lambros, Ray Luo
Membrane proteins, due to their roles as cell receptors and signaling mediators, make prime candidates for drug targets. The computational analysis of protein-ligand binding affinities has been widely employed as a tool in rational drug design efforts. Although efficient implicit solvent-based methods for modeling globular protein-ligand binding have been around for many years, the extension of such methods to membrane protein-ligand binding is still in its infancy. In this study, we extended the widely used Amber/MMPBSA method to model membrane protein-ligand systems, and we used it to analyze protein-ligand binding for the human purinergic platelet receptor (P2Y12R), a prominent drug target in the inhibition of platelet aggregation for the prevention of myocardial infarction and stroke...
December 8, 2016: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/27933962/design-synthesis-and-pharmacological-characterization-of-2-2-furanyl-thiazolo-5-4-d-pyrimidine-5-7-diamine-derivatives-new-highly-potent-a2a-adenosine-receptor-inverse-agonists-with-antinociceptive-activity
#17
Flavia Varano, Daniela Catarzi, Fabrizio Vincenzi, Marco Betti, Matteo Falsini, Annalisa Ravani, Pier Andrea Borea, Vittoria Colotta, Katia Varani
In this study, we describe the design and synthesis of new N(5)-substituted-2-(2-furanyl) thiazolo[5,4-d]pyrimidine-5,7-diamines (2-18) and their pharmacological characterization as A2A adenosine receptor (AR) antagonists by using in vitro and in vivo assays. In competition binding experiments two derivatives (13 and 14) emerged as outstanding ligands showing two different affinity values (KH and KL) for the hA2A receptor with the high affinity KH value in the femtomolar range. The in vitro functional activity assays, performed by using cyclic AMP experiments, assessed that they behave as potent inverse agonists at the hA2A AR...
December 8, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27933810/structure-based-scaffold-repurposing-for-g-protein-coupled-receptors-transformation-of-adenosine-derivatives-into-5ht2b-5ht2c-serotonin-receptor-antagonists
#18
Dilip K Tosh, Antonella Ciancetta, Eugene Warnick, Steven Crane, Zhan-Guo Gao, Kenneth A Jacobson
Adenosine derivatives developed to activate adenosine receptors (ARs) revealed micromolar activity at serotonin 5HT2B and 5HT2C receptors (5HTRs). We explored the structure-activity relationship at 5HT2Rs and modeled receptor interactions in order to optimize affinity and simultaneously reduce AR affinity. Depending on N(6) substitution, small 5'-alkylamide modification maintained 5HT2BR affinity, which was enhanced upon ribose substitution with rigid bicyclo[3.1.0]hexane (North (N)-methanocarba), e.g., N(6)-dicyclopropylmethyl 4'-CH2OH derivative 14 (Ki 11 nM)...
December 9, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27933809/development-and-validation-of-a-computational-model-for-androgen-receptor-activity
#19
Nicole C Kleinstreuer, Patricia Ceger, Eric D Watt, Matthew Martin, Keith Houck, Patience Browne, Russell S Thomas, Warren M Casey, David J Dix, David Allen, Srilatha Sakamuru, Menghang Xia, Ruili Huang, Richard Judson
Testing thousands of chemicals to identify potential androgen receptor (AR) agonists or antagonists would cost millions of dollars and take decades to complete using current validated methods. High-throughput in vitro screening (HTS) and computational toxicology approaches can more rapidly and inexpensively identify potential androgen-active chemicals. We integrated 11 HTS ToxCast/Tox21 in vitro assays into a computational network model to distinguish true AR pathway activity from technology-specific assay interference...
December 9, 2016: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/27933574/-long-term-hrv-analysis-shows-stress-reduction-by-magnesium-intake
#20
Elmar Wienecke, Claudia Nolden
BACKGROUND: Mental pressure and stress represent an ever-increasing socio-political challenge. The heart rate variability (HRV) measurement, which has its origin in the cardiac function diagnosis, gives information on the neurovegetative activity. A low HRV shows an imbalance of the sympathetic and parasympathetic efferents and thus is an indicator of stress. METHOD: A randomized, controlled, two-armed parallel study with 100 participants and a period of 90 days was performed...
December 2016: MMW Fortschritte der Medizin
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