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https://www.readbyqxmd.com/read/28350885/glutamate-dependent-ectodomain-shedding-of-neuregulin-1-type-ii-precursors-in-rat-forebrain-neurons
#1
Yuriko Iwakura, Ran Wang, Naoko Inamura, Kazuaki Araki, Shigeki Higashiyama, Nobuyuki Takei, Hiroyuki Nawa
The neurotrophic factor neuregulin 1 (NRG1) regulates neuronal development, glial differentiation, and excitatory synapse maturation. NRG1 is synthesized as a membrane-anchored precursor and is then liberated by proteolytic processing or exocytosis. Mature NRG1 then binds to its receptors expressed by neighboring neurons or glial cells. However, the molecular mechanisms that govern this process in the nervous system are not defined in detail. Here we prepared neuron-enriched and glia-enriched cultures from embryonic rat neocortex to investigate the role of neurotransmitters that regulate the liberation/release of NRG1 from the membrane of neurons or glial cells...
2017: PloS One
https://www.readbyqxmd.com/read/28350712/effect-of-knee-joint-angle-and-contraction-intensity-on-hamstrings-coactivation
#2
Rui Wu, Eamonn Delahunt, Massimiliano Ditroilo, Madeleine Lowery, Giuseppe De Vito
PURPOSE: This study investigated the effect of knee joint angle and contraction intensity on the co-activation of the hamstring muscles (when acting as antagonists to the quadriceps) in young and older individuals of both sexes. METHODS: 25 young (24 ± 2.6 years) and 26 older (70 ± 2.5 years) healthy men and women participated. Maximal voluntary isometric contraction (MVIC) of the knee extensors (KE) and flexors was assessed at two knee joint angles (90° and 60°, 0° = full extension)...
March 27, 2017: Medicine and Science in Sports and Exercise
https://www.readbyqxmd.com/read/28346715/cabergoline-related-impulse-control-disorder-in-an-adolescent-with-a-giant-prolactinoma
#3
C Bulwer, R Conn, A Shankar, F Ferrau, S Kapur, A Ederies, M Korbonits, H A Spoudeas
Giant prolactinomas, rare in children, can have devastating endocrine, neurological and visual sequelae. Dopamine agonists (DA) are effective first-line therapy with few side-effects at doses usually used for prolactinoma treatment(1) , but higher-dose therapy for Parkinson's disease has well-recognized associations with impulse control disorders (ICD) including pathological gambling, impulsive eating, compulsive shopping and hypersexuality. Such associations are not well recognized with prolactinomas; to our knowledge this is the first reported case of hypersexuality in an adolescent receiving cabergoline for a giant prolactinoma...
March 27, 2017: Clinical Endocrinology
https://www.readbyqxmd.com/read/28346520/downregulation-of-mir-139-5p-contributes-to-the-antiapoptotic-effect-of-liraglutide-on-the-diabetic-rat-pancreas-and-ins-1-cells-by-targeting-irs1
#4
Jin Li, Lei Su, Ying-Ying Gong, Mei-Lin Ding, Shu-Bin Hong, Shuang Yu, Hai-Peng Xiao
Liraglutide is administered as glucagon-like peptide-1 (GLP-1) receptor agonist for diabetic patients and can protect pancreatic β-cells by inhibiting their apoptosis. MicroRNA-139-5p (miRNA-139-5p) participates in the regulation of cancer cell apoptosis. However, it is not clear whether miR-139-5p contributes to the anti-apoptotic effect of liraglutide in β-cells. The objective of the present study was to investigate the role of miR-139-5p on apoptosis of pancreatic β-cells. MicroRNA levels in pancreatic tissue from diabetic rats and INS-1 cells treated with liraglutide were measured by real-time quantitative RT-PCR...
2017: PloS One
https://www.readbyqxmd.com/read/28346464/sympathetic-nervous-system-activity-and-anti-lipolytic-response-to-iv-glucose-load-in-subcutaneous-adipose-tissue-of-obese-and-obese-type-2-diabetic-subjects
#5
Uwe Schumann, Christopher P Jenkinson, Andreas Alt, Martina Zügel, Jürgen M Steinacker, Marion Flechtner-Mors
The study aim was to investigate the effect of endogenous insulin release on lipolysis in subcutaneous adipose tissue after adrenergic stimulation in obese subjects diagnosed with type 2 diabetes (T2D). In 14 obese female T2D subjects, or 14 obese non-T2D controls, glycerol concentration was measured in response to the α1,2,ß-agonist norepinephrine, the α1-agonist norfenefrine and the ß2-agonist terbutaline (each 10-4 M), using the microdialysis technique. After 60 minutes of stimulation, an intravenous glucose load (0...
2017: PloS One
https://www.readbyqxmd.com/read/28346226/a-tlr9-dependent-checkpoint-governs-b-cell-responses-to-dna-containing-antigens
#6
Vishal J Sindhava, Michael A Oropallo, Krishna Moody, Martin Naradikian, Lauren E Higdon, Lin Zhou, Arpita Myles, Nathaniel Green, Kerstin Nündel, William Stohl, Amanda M Schmidt, Wei Cao, Stephanie Dorta-Estremera, Taku Kambayashi, Ann Marshak-Rothstein, Michael P Cancro
Mature B cell pools retain a substantial proportion of polyreactive and self-reactive clonotypes, suggesting that activation checkpoints exist to reduce the initiation of autoreactive B cell responses. Here, we have described a relationship among the B cell receptor (BCR), TLR9, and cytokine signals that regulate B cell responses to DNA-containing antigens. In both mouse and human B cells, BCR ligands that deliver a TLR9 agonist induce an initial proliferative burst that is followed by apoptotic death. The latter mechanism involves p38-dependent G1 cell-cycle arrest and subsequent intrinsic mitochondrial apoptosis and is shared by all preimmune murine B cell subsets and CD27- human B cells...
March 27, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28346099/development-of-novel-cell-lines-for-high-throughput-screening-to-detect-estrogen-related-receptor-alpha-modulators
#7
Christina T Teng, Jui-Hua Hsieh, Jinghua Zhao, Ruili Huang, Menghang Xia, Negin Martin, Xiaohua Gao, Darlene Dixon, Scott S Auerbach, Kristine L Witt, B Alex Merrick
Estrogen-related receptor alpha (ERRα), the first orphan nuclear receptor discovered, is crucial for the control of cellular energy metabolism. ERRα and its coactivator, peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), are required for rapid energy production in response to environmental challenges. They have been implicated in the etiology of metabolic disorders such as type 2 diabetes and metabolic syndrome. ERRα also plays a role in the pathogenesis of breast cancer. Identification of compounds that modulate ERRα signaling may elucidate environmental factors associated with these diseases...
January 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28345809/effect-of-lorcaserin-on-glycemic-parameters-in-patients-with-type-2-diabetes-mellitus
#8
Faidon Magkos, Elena Nikonova, Randi Fain, Sharon Zhou, Tony Ma, William Shanahan
OBJECTIVE: Lorcaserin, a 5-HT2C receptor agonist approved for chronic weight management, is also associated with improvements in glycemic parameters in patients with/without type 2 diabetes mellitus (T2DM), but the extent to which these effects are mediated by weight loss is unknown. This post hoc analysis further examines glycemic data from the Phase III BLOOM-DM study stratified by weight changes. METHODS: Patients with T2DM were randomized to lorcaserin 10 mg twice daily or placebo...
March 27, 2017: Obesity
https://www.readbyqxmd.com/read/28345745/in-vitro-and-in-vivo-assessment-of-the-abuse-potential-of-pf614-a-novel-bio-md%C3%A2-prodrug-of-oxycodone
#9
D Lynn Kirkpatrick, William K Schmidt, Ricardo Morales, John Cremin, Julie Seroogy, Craig Husfeld, Thomas Jenkins
OBJECTIVE: The need for pain medication which will not lead to abuse is well recognized. Ensysce has designed prodrug analogs of the commonly used pain medications including hydromorphone, oxycodone (OC), hydrocodone, and morphine that limit their use to oral delivery, two of which are in clinical development. This study was undertaken to demonstrate that PF614, an extended-release prodrug of OC, allows the release of OC as designed when delivered orally, yet it resists ex vivo extraction with household chemicals and is pharmacologically inactive when administered by nonoral routes (nasal and parenteral), thereby substantially reducing its intravenous (IV) and intranasal abuse potential...
January 2017: Journal of Opioid Management
https://www.readbyqxmd.com/read/28345385/activation-of-5-ht1a-receptors-in-the-rat-dorsomedial-hypothalamus-inhibits-stress-induced-activation-of-the-hypothalamic-pituitary-adrenal-axis
#10
Christopher E Stamper, James E Hassell, Adam J Kapitz, Kenneth J Renner, Miles Orchinik, Christopher A Lowry
Acute activation of the hypothalamic-pituitary-adrenal (HPA) axis, leading to the release of corticosteroid hormones into the circulation, is an adaptive response to perceived threats. Persistent activation of the HPA axis can lead to impaired physiological or behavioral function with maladaptive consequences. Thus, efficient control and termination of stress responses is essential for well-being. However, inhibitory control mechanisms governing the HPA axis are poorly understood. Previous studies suggest that serotonergic systems, acting within the medial hypothalamus, play an important role in inhibitory control of stress-induced HPA axis activity...
March 27, 2017: Stress: the International Journal on the Biology of Stress
https://www.readbyqxmd.com/read/28345052/cardiac-myosin-binding-protein-c-ser-302-phosphorylation-regulates-cardiac-%C3%AE-adrenergic-reserve
#11
Ranganath Mamidi, Kenneth S Gresham, Jiayang Li, Julian E Stelzer
Phosphorylation of cardiac myosin binding protein-C (MyBP-C) modulates cardiac contractile function; however, the specific roles of individual serines (Ser) within the M-domain that are targets for β-adrenergic signaling are not known. Recently, we demonstrated that significant accelerations in in vivo pressure development following β-agonist infusion can occur in transgenic (TG) mouse hearts expressing phospho-ablated Ser(282) (that is, TG(S282A)) but not in hearts expressing phospho-ablation of all three serines [that is, Ser(273), Ser(282), and Ser(302) (TG(3SA))], suggesting an important modulatory role for other Ser residues...
March 2017: Science Advances
https://www.readbyqxmd.com/read/28345002/cxcl12-promotes-stem-cell-recruitment-and-uterine-repair-after-injury-in-asherman-s-syndrome
#12
Gulcin Sahin Ersoy, Masoumeh Majidi Zolbin, Emine Cosar, Irene Moridi, Ramanaiah Mamillapalli, Hugh S Taylor
Asherman's syndrome is an acquired condition of uterine fibrosis and adhesions in response to injury that adversely affects fertility and pregnancy. We have previously demonstrated that bone marrow-derived mesenchymal stem cells (BMDSCs) contribute to uterine repair after injury and that stem cells supplementation improves fertility. Here, we demonstrate that CXCL12 is the chemokine that mediates stem cell engraftment and functional improvement using a murine model of Asherman's syndrome. After uterine injury, we demonstrate that CXCL12 augmentation increased BMDSC engraftment and that the CXCL12 receptor (CXCR4) antagonist, ADM3100, blocked stem cell recruitment...
March 17, 2017: Molecular Therapy. Methods & Clinical Development
https://www.readbyqxmd.com/read/28344969/catamenial-hemoptysis-accompanied-by-subcutaneous-endometriosis-treated-with-combination-therapy
#13
Hye-In Jang, Sung-Eun Kim, Tae-Joong Kim, Yoo-Young Lee, Chel-Hun Choi, Jeong-Won Lee, Byoung-Gie Kim, Duk-Soo Bae
Extra pelvic endometriosis is considered to be rare. This paper reports a case of catamenial hemoptysis accompanied by subcutaneous endometriosis in 26-year-old woman. A computed tomography scan of the chest revealed a focal ground-glass opacity lesion in the posterior segment of the right upper lobe. Histopathology confirmed the diagnosis of endometriosis of right lung and concurrent subcutaneous endometriosis. She was treated with surgical resection of the endometriosis lesions on two different sites and perioperative gonadotropin-releasing hormone agonist therapy...
March 2017: Obstetrics & Gynecology Science
https://www.readbyqxmd.com/read/28344961/recurrence-factors-and-reproductive-outcomes-of-laparoscopic-myomectomy-and-minilaparotomic-myomectomy-for-uterine-leiomyomas
#14
Dong Gi Shin, Heon Jong Yoo, Yeon Ah Lee, In Sun Kwon, Ki Hwan Lee
OBJECTIVE: The aim of this study was to determine recurrence factors and reproductive outcomes of laparoscopic myomectomy (LM) and minilaparotomic myomectomy (MM) for treating uterine leiomyomas. METHODS: Between 2007 and 2013, 160 patients underwent myomectomy, including 122 who underwent LM and 38 who underwent MM. Patients were followed up for recurrence based on pelvic ultrasound exams. Only patients who were followed up for a minimum of two years were selected for this retrospective study...
March 2017: Obstetrics & Gynecology Science
https://www.readbyqxmd.com/read/28344813/the-modern-role-of-androgen-deprivation-therapy-in-the-management-of-localised-and-locally-advanced-prostate-cancer
#15
Charlotte Gunner, Aziz Gulamhusein, Derek J Rosario
INTRODUCTION: Approximately 50% of men diagnosed with prostate cancer will be exposed to androgen deprivation therapy (ADT) at some stage. The role of ADT in the management of metastatic disease has long been recognised, and its place in the management of localised and locally advanced disease has become clearer in the past few years. Nevertheless, concerns remain that some men might not benefit from ADT in earlier-stage disease. The purpose of the current article is to provide a brief narrative review of the role of ADT as part of a strategy of treatment with curative intent, concentrating mainly on key recent developments in the area...
December 2016: Journal of Clinical Urology
https://www.readbyqxmd.com/read/28344789/a-ppar-gamma-agonist-protects-from-radiation-induced-intestinal-toxicity
#16
Monica Mangoni, Mariangela Sottili, Chiara Gerini, Isacco Desideri, Cinzia Bastida, Stefania Pallotta, Francesca Castiglione, Pierluigi Bonomo, Icro Meattini, Daniela Greto, Sabrina Cappelli, Lucia Di Brina, Mauro Loi, Giampaolo Biti, Lorenzo Livi
OBJECTIVE: Because of its anti-inflammatory, anti-fibrotic, anti-apoptotic and anti-neoplastic properties, the PPAR-γ agonist rosiglitazone is an interesting drug for investigating for use in the prevention and treatment of radiation-induced intestinal damage. We aimed to evaluate the radioprotective effect of rosiglitazone in a murine model of acute intestinal damage, assessing whether radioprotection is selective for normal tissues or also occurs in tumour cells. METHODS: Mice were total-body irradiated (12 Gy), with or without rosiglitazone (5 mg/kg/day)...
March 2017: United European Gastroenterology Journal
https://www.readbyqxmd.com/read/28344445/effects-of-static-and-dynamic-stretching-on-the-isokinetic-peak-torques-and-electromyographic-activities-of-the-antagonist-muscles
#17
Abdullah Serefoglu, Ufuk Sekir, Hakan Gür, Bedrettin Akova
The aim of this study was to investigate if static and dynamic stretching exercises of the knee muscles (quadriceps and hamstring muscles) have any effects on concentric and eccentric isokinetic peak torques and electromyographic amplitudes (EMG) of the antagonist muscles. Twenty healthy male athletes (age between 18-30 years) voluntarily participated in this study. All of the subjects visited the laboratory to complete the following intervention in a randomized order on 5 separate days; (a) non-stretching (control), (b) static stretching of the quadriceps muscles, (c) static stretching of the hamstring muscles, (d) dynamic stretching of the quadriceps muscles, and (e) dynamic stretching of the hamstring muscles...
March 2017: Journal of Sports Science & Medicine
https://www.readbyqxmd.com/read/28344125/capadenoson-a-clinically-trialed-partial-adenosine-a1-receptor-agonist-can-stimulate-adenosine-a2b-receptor-biased-agonism
#18
Jo-Anne Baltos, Elizabeth A Vecchio, Matthew A Harris, Cheng Xue Qin, Rebecca H Ritchie, Arthur Christopoulos, Paul J White, Lauren T May
The adenosine A2B receptor (A2BAR) has been identified as an important therapeutic target in cardiovascular disease, however in vitro and in vivo targeting has been limited by the paucity of pharmacological tools, particularly potent agonists. Interestingly, 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)-2-pyridinyl)thio)acetamide (BAY60-6583), a potent and subtype-selective A2BAR agonist, has the same core structure as 2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitril (capadenoson)...
March 23, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28344112/efficacy-and-safety-of-once-weekly-semaglutide-versus-once-daily-insulin-glargine-as-add-on-to-metformin-with-or-without-sulfonylureas-in-insulin-naive-patients-with-type-2-diabetes-sustain-4-a-randomised-open-label-parallel-group-multicentre-multinational
#19
Vanita R Aroda, Stephen C Bain, Bertrand Cariou, Milivoj Piletič, Ludger Rose, Mads Axelsen, Everton Rowe, J Hans DeVries
BACKGROUND: Several pharmacological treatment options are available for type 2 diabetes; however, many patients do not achieve optimum glycaemic control and therefore new therapies are necessary. We assessed the efficacy and safety of semaglutide, a glucagon-like peptide-1 (GLP-1) analogue in clinical development, compared with insulin glargine in patients with type 2 diabetes who were inadequately controlled with metformin (with or without sulfonylureas). METHODS: We did a randomised, open-label, non-inferiority, parallel-group, multicentre, multinational, phase 3a trial (SUSTAIN 4) at 196 sites in 14 countries...
March 23, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28343901/gper-blockers-as-nox-downregulators-a-new-drug-class-to-target-chronic-non-communicable-diseases
#20
Matthias R Meyer, Matthias Barton
Oxidative stress is a hallmark of chronic non-communicable diseases such as arterial hypertension, diabetes, coronary artery disease, and stroke. Cardiovascular diseases are characterized by increased production of reactive oxygen species (ROS) by NAPDH oxidase 1 (Nox1) and additional Nox isoforms among other sources. Activation of the G protein-coupled estrogen receptor (GPER) can mediate multiple salutary effects on the cardiovascular system. However, GPER also has constitutive activity, e.g. in the absence of specific agonists, that was recently shown to promote hypertension and aging-induced tissue damage by enabling Nox1-derived production of ROS...
March 23, 2017: Journal of Steroid Biochemistry and Molecular Biology
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