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https://www.readbyqxmd.com/read/28109183/chloride-ion-transport-and-overexpression-of-tmem16a-in-a-guinea-pig-asthma-model
#1
Mitsuko Kondo, Mayoko Tsuji, Kaori Hara, Ken Arimura, Osamitsu Yagi, Etsuko Tagaya, Kiyoshi Takeyama, Jun Tamaoki
BACKGROUND: TMEM16A, a Ca-activated Cl channel, regulates various physiological functions such as mucin secretion. However, the role of TMEM16A in hypersecretion in asthma is not fully understood. OBJECTIVE: The aim of this study is to evaluate Cl ion transport via TMEM16A and determine the localization of TMEM16A in a guinea pig asthma model. METHODS: Guinea pigs were sensitized with OVA ip. on Day 1 and Day 8. On Day 22, we assessed OVA challenge-induced Cl ion transport in the sensitized tracheas ex vivo in an Ussing chamber, compared with the non-sensitized tracheas...
January 21, 2017: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28109166/a-novel-dual-amylin-and-calcitonin-receptor-agonist-dacra-kbp-089-induces-weight-loss-through-a-reduction-in-fat-but-not-lean-mass-while-improving-food-preference
#2
Sofie Gydesen, Sara Toftegaard Hjuler, Zenia Freving, Kim Vietz Andreassen, Nina Sonne, Lars I Hellgren, Morten Asser Karsdal, Kim Henriksen
BACKGROUND AND PURPOSE: Obesity and associated co-morbidities, such as type 2 diabetes and non-alcoholic fatty liver disease, are major health challenges - hence, development of weight loss therapies with the ability to reduce the co-morbidities is key. EXPERIMENTAL APPROACH: The effect of the dual amylin and calcitonin receptor agonist (DACRA), KBP-089, on bodyweight, glucose homeostasis, and fatty acid accumulation in liver and muscle tissue, food preference was investigated...
January 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28109164/assessment-of-biological-psychological-and-adherence-factors-in-the-prediction-of-step-down-treatment-for-patients-with-well-controlled-asthma
#3
Norihiro Saito, Akihito Kamata, Masamichi Itoga, Mami Tamaki, Hiroyuki Kayaba, Thomas Ritz
OBJECTIVES: Inhaled corticosteroids (ICS) and inhaled corticosteroids combined with long-acting beta2-agonist (ICS/LABA) are standard treatments for asthma. However, factors that might help reduce medication in well-controlled asthma are unknown. We classified problems of asthma patients into biological, psychological and adherence factors, and investigated factors associated with the indication and failure of a medication step-down treatment. METHODS: Two hundred twenty two well-controlled asthma patients receiving ICS or ICS/LABA were assessed for physical and psychiatric problems and followed up for one year from adjustment of their treatment step...
January 21, 2017: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28109139/-imiquimod-combined-with-dendritic-cell-vaccine-decreases-treg-proportion-and-enhances-anti-tumor-responses-in-mice-bearing-melanoma
#4
Shurong Ren, Qiubo Wang, Yanli Zhang, Cuixiu Lu, Ping Li, Yumei Li
Objective To investigate the therapeutic effect of Toll-like receptor 7 (TLR7) agonist imiquimod combined with dendritic cell (DC)-based tumor vaccine on melanoma in mice and the potential mechanism. Methods Melanoma-bearing mouse models were established by subcutanous injection of B16-OVA cells into C57BL/6 mice. DCs were isolated from mouse bone marrow and propagated in culture medium with recombinant mouse granulocyte-macrophage colony-stimulating factor (rmGM-CSF) and recombinant mouse interleukin-4 (rmIL-4)...
February 2017: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/28109061/urocortin-suppresses-endometrial-cancer-cell-migration-via-crfr2-and-its-system-components-are-differentially-modulated-by-estrogen
#5
Gemma L Owens, Kevin M Lawrence, Tom R Jackson, Emma J Crosbie, Berna S Sayan, Henry C Kitchener, Paul A Townsend
Urocortin (UCN1) peptide shares structural and functional homology with corticotropin-releasing factor (CRF). UCN1 is significantly reduced in endometrial adenocarcinoma compared to healthy controls. However, there are no data which evaluate the effects of UCN1 in the endometrium, or how it is modulated. We used proliferation and transwell assays to determine the effect of UCN1 on the proliferation and migration of Ishikawa and HEC1A cells. We also determined the expression levels of UCN1 and its receptors produced by estrogen receptor agonists, and the effect of UCN1 on estrogen receptor expression, using quantitative polymerase chain reaction...
January 21, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28109047/novel-antiplatelet-role-for-a-protein-disulfide-isomerase-targeted-peptide-evidence-of-covalent-binding-to-c-terminal-cghc-redox-motif
#6
H R Sousa, R S Gaspar, E M L Sena, S A da Silva, J L de L Fontelles, T L S Araújo, M Mastrogiovanni, D M Fries, A P S Azevedo-Santos, F R M Laurindo, A Trostchansky, A M Paes
Protein disulfide isomerase (PDI) plays a major role in platelet aggregation and its inhibitors have emerged as novel antithrombotic drugs. In previous work, we designed a peptide based on PDI redox motif (CGHC) that inhibited both PDI reductase activity and PDI-modulated superoxide generation by neutrophil Nox2. Thus, we hypothesized this peptide would also inhibit platelet aggregation by association to surface PDI. Three peptides were used: CxxC, containing the PDI redox motif; Scr, presenting a scrambled sequence of the same residues and AxxA, with cysteines replaced by alanine...
January 21, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28108665/fasiglifam-tak-875-alters-bile-acid-homeostasis-in-rats-and-dogs-a-potential-cause-of-drug-induced-liver-injury
#7
Francis S Wolenski, Andy Z X Zhu, Mike Johnson, Shaoxia Yu, Yuu Moriya, Takuya Ebihara, Vilmos Csizmadia, Jessica Grieves, Martin Paton, Mingxiang Liao, Christopher Gemski, Liping Pan, Majid Vakilynejad, Yvonne P Dragan, Swapan K Chowdhury, Patrick J Kirby
Fasiglifam (TAK-875), a Free Fatty Acid Receptor 1 (FFAR1) agonist in development for the treatment of type 2 diabetes, was voluntarily terminated in phase 3 due to adverse liver effects. A mechanistic investigation described in this manuscript focused on the inhibition of bile acid (BA) transporters as a driver of the liver findings. TAK-875 was an in vitro inhibitor of multiple influx (NTCP and OATPs) and efflux (BSEP and MRPs) hepatobiliary BA transporters at micromolar concentrations. Repeat dose studies determined that TAK-875 caused a dose-dependent increase in serum total BA in rats and dogs...
January 20, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28108647/effects-of-early-life-exposure-to-thip-on-brainstem-neuronal-excitability-in-the-mecp2-null-mouse-model-of-rett-syndrome-before-and-after-drug-withdrawal
#8
Weiwei Zhong, Christopher M Johnson, Ningren Cui, Max F Oginsky, Yang Wu, Chun Jiang
Rett syndrome (RTT) is mostly caused by mutations of the X-linked MECP2 gene. Although the causal neuronal mechanisms are still unclear, accumulating experimental evidence obtained from Mecp2(-/Y) mice suggests that imbalanced excitation/inhibition in central neurons plays a major role. Several approaches may help to rebalance the excitation/inhibition, including agonists of GABAA receptors (GABAAR). Indeed, our previous studies have shown that early-life exposure of Mecp2-null mice to the extrasynaptic GABAAR agonist THIP alleviates several RTT-like symptoms including breathing disorders, motor dysfunction, social behaviors, and lifespan...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28108622/a-genome-wide-loss-of-function-screen-identifies-slc26a2-as-a-novel-mediator-of-trail-resistance
#9
Lina Dimberg, Christina G Towers, Kian Behbakht, Taylor Hotz, Jihye Kim, Susan P Fosmire, Christopher C Porter, Aik-Choon Tan, Andrew Thorburn, Heide L Ford
: TNF-related apoptosis inducing ligand (TRAIL) is a potent death-inducing ligand that mediates apoptosis through the extrinsic pathway and serves as an important endogenous tumor suppressor mechanism. Because tumor cells are often killed by TRAIL and normal cells are not, drugs that activate the TRAIL pathway have been thought to have potential clinical value. However, to date, most TRAIL-related clinical trials have largely failed due to the tumor cells having intrinsic or acquired resistance to TRAIL-induced apoptosis...
January 20, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28108512/constitutive-notch3-signaling-promotes-the-growth-of-basal-breast-cancers
#10
Lisa Choy, Thijs Hagenbeek, Margaret Solon, Dorothy M French, David Finkle, Amy Shelton, Rayna Venook, Matthew J Brauer, Christian W Siebel
Notch ligands signal through one of four receptors on neighboring cells to mediate cell-cell communication and control cell fate, proliferation and survival. Although aberrant Notch activation has been implicated in numerous malignancies, including breast cancer, the importance of individual receptors in distinct breast cancer subtypes and the mechanisms of receptor activation remain unclear. Using a novel antibody to detect active NOTCH3, we report here that NOTCH3 signals constitutively in a panel of basal breast cancer cell lines and in more than one-third of basal tumors...
January 20, 2017: Cancer Research
https://www.readbyqxmd.com/read/28108498/mglur2-versus-mglur3-metabotropic-glutamate-receptors-in-primate-dorsolateral-prefrontal-cortex-postsynaptic-mglur3-strengthen-working-memory-networks
#11
Lu E Jin, Min Wang, Veronica C Galvin, Taber C Lightbourne, Peter Jeffrey Conn, Amy F T Arnsten, Constantinos D Paspalas
The newly evolved circuits in layer III of primate dorsolateral prefrontal cortex (dlPFC) generate the neural representations that subserve working memory. These circuits are weakened by increased cAMP-K(+) channel signaling, and are a focus of pathology in schizophrenia, aging, and Alzheimer's disease. Cognitive deficits in these disorders are increasingly associated with insults to mGluR3 metabotropic glutamate receptors, while reductions in mGluR2 appear protective. This has been perplexing, as mGluR3 has been considered glial receptors, and mGluR2 and mGluR3 have been thought to have similar functions, reducing glutamate transmission...
January 19, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28108357/sigma-1-receptor-deficiency-reduces-gabaergic-inhibition-in-the-basolateral-amygdala-leading-to-ltd-impairment-and-depressive-like-behaviors
#12
Baofeng Zhang, Ling Wang, Tingting Chen, Juan Hong, Sha Sha, Jun Wang, Hang Xiao, Ling Chen
Sigma-1 receptor knockout (σ1R-/-) in male mice causes depressive-like phenotype. We observed the expression of σ1R in principal neurons of basolateral amygdala (BLA), a main region for affective regulation. The present study investigated the influence of σ1R deficiency in BLA neurons on synaptic properties and plasticity at cortico-BLA pathway. In comparison with wild-type (WT) mice, the slopes of field excitatory postsynaptic potentials (fEPSP) were reduced in σ1R-/- mice with the increases in paired-pulse facilitation (PPF) and paired-pulse inhibition (PPI) values...
January 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28108356/lipid-a-structural-modifications-in-extreme-conditions-and-identification-of-unique-modifying-enzymes-to-define-the-toll-like-receptor-4-structure-activity-relationship
#13
REVIEW
Alison J Scott, Benjamin L Oyler, David R Goodlett, Robert K Ernst
Strategies utilizing Toll-like receptor 4 (TLR4) agonists for treatment of cancer, infectious diseases, and other targets report promising results. Potent TLR4 antagonists are also gaining attention as therapeutic leads. Though some principles for TLR4 modulation by lipid A have been described, a thorough understanding of the structure-activity relationship (SAR) is lacking. Only through a complete definition of lipid A-TLR4 SAR is it possible to predict TLR4 signaling effects of discrete lipid A structures, rendering them more pharmacologically relevant...
January 17, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28108028/comparison-of-ca-2-puffs-evoked-by-extracellular-agonists-and-photoreleased-ip3
#14
REVIEW
Jeffrey T Lock, Ian F Smith, Ian Parker
The inositol trisphosphate (IP3) signaling pathway evokes local Ca(2+) signals (Ca(2+) puffs) that arise from the concerted openings of clustered IP3 receptor/channels in the ER membrane. Physiological activation is triggered by binding of agonists to G-protein-coupled receptors (GPCRs) on the cell surface, leading to cleavage of phosphatidyl inositol bisphosphate and release of IP3 into the cytosol. Photorelease of IP3 from a caged precursor provides a convenient and widely employed means to study the final stage of IP3-mediated Ca(2+) liberation, bypassing upstream signaling events to enable more precise control of the timing and relative concentration of cytosolic IP3...
December 5, 2016: Cell Calcium
https://www.readbyqxmd.com/read/28107913/quantitative-structure-retention-relationship-model-for-the-determination-of-naratriptan-hydrochloride-and-its-impurities-based-on-artificial-neural-networks-coupled-with-genetic-algorithm
#15
Mikołaj Mizera, Anna Krause, Przemysław Zalewski, Robert Skibiński, Judyta Cielecka-Piontek
Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed automated method of creation Quantitative Structure-Retention Relationship (QSRR) for analysis of triptans, selective serotonin 5-HT1 receptor agonists used for the treatment of acute headache. The method was created using hybrid machine learning approach, namely Genetic algorithm (GA) coupled with artificial neutral networks (ANN)...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28107868/effect-of-ppar%C3%AE-agonist-rosiglitazone-on-the-secretion-of-th2-cytokine-in-asthma-mice
#16
Ji-Hui Yu, Li Long, Zhi-Xiao Luo, Jie-Ru You
OBJECTIVE: To explore the effect of PPARγ agonist (rosiglitazone) on the secretion of Th2 cytokines and the proportion of immune cell subsets in asthma mice. METHODS: Ovalbumin (OVA)-sensitized mice were used to build asthma models. Those mice were divided into the normal control group, model group and rosiglitazone group. Differences of the changes in lung histopathology of mice in the three groups were observed through hematoxylin and eosin (HE) strain, and the numbers of the total cells, eosinophils and neutrophils in BALF of mice in the three groups were compared...
January 2017: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/28107824/implementation-of-methadone-therapy-for-opioid-use-disorder-in-russia-a-modeled-cost-effectiveness-analysis
#17
Bulat Idrisov, Sean M Murphy, Tyler Morrill, Mayada Saadoun, Karsten Lunze, Donald Shepard
BACKGROUND: Opioid agonist therapy using methadone, an effective treatment of opioid use disorders (OUD) for people who inject drugs (PWID), is recommended by the World Health Organization as essential to curtail the growing HIV epidemic. Yet, despite increasing prevalence of OUD and HIV, methadone therapy has not yet been implemented in Russia. The aim of this modeling study was to estimate the cost-effectiveness of methadone therapy for Russian adults with a diagnosed OUD. METHODS/DESIGN: We modeled the projected program implementation costs and estimated disability-adjusted life years (DALYs) averted over a 10-year period, associated with the provision of methadone therapy for a hypothetical, unreplenished cohort of Russian adults with an OUD (n = 249,000), in comparison to the current therapies at existing addiction treatment facilities...
January 20, 2017: Substance Abuse Treatment, Prevention, and Policy
https://www.readbyqxmd.com/read/28107783/lorcaserin-suppresses-oxycodone-self-administration-and-relapse-vulnerability-in-rats
#18
Harshini Neelakantan, Erica D Holliday, Robert G Fox, Sonja J Stutz, Sandra D Comer, Margaret Haney, Noelle C Anastasio, Frederick Gerard Moeller, Kathryn A Cunningham
Opioid use disorder (OUD) is a major public health problem. High relapse rates and poor treatment retention continue to pose major challenges in OUD treatment. Of the abused opioids, oxycodone is well described to maintain self-administration and evoke the durable conditioned responses ("cue reactivity") that result from pairing of opioid-related stimuli (e.g., paraphernalia) with repeated abuse. Serotonin (5-HT) neurotransmission, particularly through the 5-HT2C receptor (5-HT2CR), regulates psychostimulant reward and cue reactivity, and in the present experiments, we investigated the hypothesis that the selective 5-HT2CR agonist lorcaserin, which is FDA-approved for the treatment of obesity, will suppress oxycodone self-administration and oxycodone-associated cue reactivity in rats...
January 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28107769/the-transcriptional-modulator-ifrd1-controls-pgc-1%C3%AE-expression-under-short-term-adrenergic-stimulation-in-brown-adipocytes
#19
Gyujin Park, Tetsuhiro Horie, Takashi Kanayama, Kazuya Fukasawa, Takashi Iezaki, Yuki Onishi, Kakeru Ozaki, Yukari Nakamura, Yukio Yoneda, Takeshi Takarada, Eiichi Hinoi
Sympathetic tone activates the function of classical brown adipocytes, which constitutively exist in the brown adipose tissue, and inducible brown adipocytes (so-called beige adipocytes), which sporadically reside within the white adipose tissue. Here we identified the transcriptional modulator interferon-related developmental regulator 1 (Ifrd1) as a negative regulator of thermogenic and mitochondrial gene expression in brown adipocytes. Ifrd1 expression was markedly induced by cold exposure and administration of CL-316243 (a β3 adrenergic agonist) in interscapular brown adipose and inguinal subcutaneous white adipose tissues, but not in epididymal visceral white adipose tissue, in vivo...
January 20, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28107494/protective-roles-for-rgs2-in-a-mouse-model-of-house-dust-mite-induced-airway-inflammation
#20
Tresa George, Matthew Bell, Mainak Chakraborty, David P Siderovski, Mark A Giembycz, Robert Newton
The GTPase-accelerating protein, regulator of G-protein signalling 2 (RGS2) reduces signalling from G-protein-coupled receptors (GPCRs) that signal via Gαq. In humans, RGS2 expression is up-regulated by inhaled corticosteroids (ICSs) and long-acting β2-adrenoceptor agonists (LABAs) such that synergy is produced in combination. This may contribute to the superior clinical efficacy of ICS/LABA therapy in asthma relative to ICS alone. In a murine model of house dust mite (HDM)-induced airways inflammation, three weeks of intranasal HDM (25 μg, 3×/week) reduced lung function and induced granulocytic airways inflammation...
2017: PloS One
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