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https://www.readbyqxmd.com/read/28432980/discovery-of-potential-inhibitor-against-human-acetylcholinesterase-a-molecular-docking-and-molecular-dynamics-investigation
#1
Surya Pratap Singh, Dwijendra Gupta
Alzheimer's disease (AD) is a progressive neurodegenerative disease of central nervous system among elderly people. Human acetylcholinesterase (hAChE), an important enzyme in neuronal signaling, is responsible for the degradation of acetylcholine which in turn prevents the post synaptic signal transmissions. hAChE has been an attractive target of drug discovery for the search of therapeutics against AD. In the recent past hAChE has become hot target for the investigation of new potential therapeutics. We performed virtual screening of entire database against hAChE...
April 12, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28432945/exploring-isoxsuprine-hydrochloride-binding-with-human-serum-albumin-in-the-presence-of-folic-acid-and-ascorbic-acid-using-multispectroscopic-and-molecular-modeling-methods
#2
Fereshteh Shiri, Somaye Shahraki, Amin Shahriyar, Mostafa Heidari Majd
Isoxsuprine hydrochloride (vasodilator drug), folic acid and ascorbic acid are medicines which can be utilized alone or simultaneously by pregnant women. In the present work the competitive binding of isoxsuprine hydrochloride (ISO) with human serum albumin (HSA) in the absence and presence of folic acid (FOL) and ascorbic acid (AS) was investigated using different spectroscopic probes and molecular docking studies. The results of fluorescence suggested that isoxsuprine alone or in the presence of ascorbic acid can bind to HSA and quench the fluorescence of HSA with static mechanism but For HSA-folic acid-isoxsuprine system, dynamic type of quenching mechanisms is involved...
April 11, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28432191/gene-expression-effects-of-glucocorticoid-and-mineralocorticoid-receptor-agonists-and-antagonists-on-normal-human-skeletal-muscle
#3
Jessica A Chadwick, James Spencer Hauck, Celso E Gomez-Sanchez, Elise P Gomez-Sanchez, Jill A Rafael-Fortney
Mineralocorticoid and glucocorticoid receptors are closely related steroid hormone receptors that regulate gene expression through many of the same hormone response elements. However, their transcriptional activities and effects in skeletal muscles are largely unknown. We recently identified mineralocorticoid receptors (MR) in skeletal muscles after finding that combined treatment with the angiotensin-converting enzyme inhibitor lisinopril and MR antagonist spironolactone was therapeutic in Duchenne muscular dystrophy mouse models...
April 21, 2017: Physiological Genomics
https://www.readbyqxmd.com/read/28432051/impact-of-study-outcome-on-submission-and-acceptance-metrics-for-peer-reviewed-medical-journals-six-year-retrospective-review-of-all-completed-glaxosmithkline-human-drug-research-studies
#4
Gary Evoniuk, Bernadette Mansi, Barbara DeCastro, Jennie Sykes
Objectives To determine whether the outcome of drug studies influenced submission and/or acceptance rates for publication in peer reviewed medical journals.Design A six year retrospective review of publication status by study outcome for all human drug research studies conducted by a single industry sponsor (GlaxoSmithKline) that completed from 1 January 2009 to 30 June 2014 and were therefore due for manuscript submission (per the sponsor's policy) to peer reviewed journals within 18 months of study completion-that is, 31 December 2015...
April 21, 2017: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/28431671/where-are-we-now-a-clinicians-guide-to-the-use-of-follow-on-insulin-for-patients-with-diabetes
#5
Steven V Edelman, Priscilla A Hollander, Eugene E Wright
Insulin has been used as a standard treatment for patients with diabetes for almost 100 years. Over time, advances in insulin development have improved its pharmacologic properties. (Online access: http://courses.elseviercme.com/t2dm/666). Most recently, the US Food and Drug Administration approved a novel, follow-on basal insulin agent, with more expected to be commercially available in the near future. With the imminent availability of follow-on basal insulin agents, clinicians need to be aware of the potential benefits and concerns in order to facilitate informed decision making and to provide the best possible advice and guidance to their patients with diabetes...
May 2017: American Journal of Medicine
https://www.readbyqxmd.com/read/28431584/monitoring-quality-and-coverage-of-harm-reduction-services-for-people-who-use-drugs-a-consensus-study
#6
Lucas Wiessing, Marica Ferri, Vendula Běláčková, Patrizia Carrieri, Samuel R Friedman, Cinta Folch, Kate Dolan, Brian Galvin, Peter Vickerman, Jeffrey V Lazarus, Viktor Mravčík, Mirjam Kretzschmar, Vana Sypsa, Ana Sarasa-Renedo, Anneli Uusküla, Dimitrios Paraskevis, Luis Mendão, Diana Rossi, Nadine van Gelder, Luke Mitcheson, Letizia Paoli, Cristina Diaz Gomez, Maitena Milhet, Nicoleta Dascalu, Jonathan Knight, Gordon Hay, Eleni Kalamara, Roland Simon, Catherine Comiskey, Carla Rossi, Paul Griffiths
BACKGROUND AND AIMS: Despite advances in our knowledge of effective services for people who use drugs over the last decades globally, coverage remains poor in most countries, while quality is often unknown. This paper aims to discuss the historical development of successful epidemiological indicators and to present a framework for extending them with additional indicators of coverage and quality of harm reduction services, for monitoring and evaluation at international, national or subnational levels...
April 22, 2017: Harm Reduction Journal
https://www.readbyqxmd.com/read/28431485/efficacy-of-golimumab-in-belgian-patients-with-active-rheumatoid-arthritis-despite-treatment-with-non-biologic-disease-modifying-anti-rheumatic-drugs-sub-analysis-of-the-go-more-study
#7
Patrick Durez, Marie Vanthuyne, Muhammad S Soyfoo, Ilse Hoffman, Michel Malaise, Piet Geusens
OBJECTIVES: The GO-MORE trial (NCT00975130) was a phase 3 study in 40 countries evaluating the efficacy and safety of golimumab as add-on therapy in biologic-naïve adults with active rheumatoid arthritis despite stable treatment with disease-modifying anti-rheumatic drugs. To inform local practice in Belgium and examine the role of baseline disease activity in treatment response, we compared the efficacy of golimumab in the Belgian subpopulation and the rest of the world. METHODS: Baseline disease activity and six-month efficacy rates in the GO-MORE trial were compared for the Belgian subpopulation and the rest of the world by t-tests and chi-squared tests...
April 21, 2017: Acta Clinica Belgica
https://www.readbyqxmd.com/read/28431202/pharmacological-interventions-for-acute-pancreatitis
#8
REVIEW
Elisabetta Moggia, Rahul Koti, Ajay P Belgaumkar, Federico Fazio, Stephen P Pereira, Brian R Davidson, Kurinchi Selvan Gurusamy
BACKGROUND: In people with acute pancreatitis, it is unclear what the role should be for medical treatment as an addition to supportive care such as fluid and electrolyte balance and organ support in people with organ failure. OBJECTIVES: To assess the effects of different pharmacological interventions in people with acute pancreatitis. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL, 2016, Issue 9), MEDLINE, Embase, Science Citation Index Expanded, and trial registers to October 2016 to identify randomised controlled trials (RCTs)...
April 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28431186/unfractionated-heparin-versus-low-molecular-weight-heparins-for-avoiding-heparin-induced-thrombocytopenia-in-postoperative-patients
#9
REVIEW
Daniela R Junqueira, Liliane M Zorzela, Edson Perini
BACKGROUND: Heparin-induced thrombocytopenia (HIT) is an adverse drug reaction presenting as a prothrombotic disorder related to antibody-mediated platelet activation. It is a paradoxical immune reaction resulting in thrombin generation in vivo, which leads to a hypercoagulable state and the potential to initiate venous or arterial thrombosis. A number of factors are thought to influence the incidence of HIT including the type and preparation of heparin (unfractionated heparin (UFH) or low molecular weight heparin (LMWH)) and the heparin-exposed patient population, with the postoperative patient population at higher risk...
April 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28430700/prescriber-compliance-with-liver-monitoring-guidelines-for-pazopanib-in-the-postapproval-setting-results-from-a-distributed-research-network
#10
Sumitra Shantakumar, Beth L Nordstrom, Susan A Hall, Luc Djousse, Myrthe P P van Herk-Sukel, Kathy H Fraeman, David R Gagnon, Karen Chagin, Jeanenne J Nelson
OBJECTIVES: Pazopanib received US Food and Drug Administration approval in 2009 for advanced renal cell carcinoma. During clinical development, liver chemistry abnormalities and adverse hepatic events were observed, leading to a boxed warning for hepatotoxicity and detailed label prescriber guidelines for liver monitoring. As part of postapproval regulatory commitments, a cohort study was conducted to assess prescriber compliance with liver monitoring guidelines. METHODS: Over a 4-year period, a distributed network approach was used across 3 databases: US Veterans Affairs Healthcare System, a US outpatient oncology community practice database, and the Dutch PHARMO Database Network...
April 20, 2017: Journal of Patient Safety
https://www.readbyqxmd.com/read/28430558/lower-esophageal-sphincter-augmentation-for-gastroesophageal-reflux-disease-the-safety-of-a-modern-implant
#11
C Daniel Smith, Robert A Ganz, John C Lipham, Reginald C Bell, David W Rattner
INTRODUCTION: Use of the magnetic sphincter augmentation device (MSAD) for gastroesophageal reflux disease (GERD) is increasing. As this innovative treatment for GERD gains widespread use and adoption, an assessment of its safety since U.S. market introduction is presented. METHODS: Events were collected from the Manufacturer and User Facility Device Experience (MAUDE) database, which reports events submitted to the Food and Drug Administration (FDA) of suspected device-associated deaths, serious injuries, and malfunctions...
April 21, 2017: Journal of Laparoendoscopic & Advanced Surgical Techniques. Part A
https://www.readbyqxmd.com/read/28430205/controlled-membrane-translocation-provides-a-mechanism-for-signal-transduction-and-amplification
#12
Matthew J Langton, Flore Keymeulen, Maria Ciaccia, Nicholas H Williams, Christopher A Hunter
Transmission and amplification of chemical signals across lipid bilayer membranes is of profound significance in many biological processes, from the development of multicellular organisms to information processing in the nervous system. In biology, membrane-spanning proteins are responsible for the transmission of chemical signals across membranes, and signal transduction is often associated with an amplified signalling cascade. The ability to reproduce such processes in artificial systems has potential applications in sensing, controlled drug delivery and communication between compartments in tissue-like constructs of synthetic vesicles...
May 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28429843/pooled-analysis-of-three-randomized-double-blind-placebo-controlled-trials-with-rimonabant-for-smoking-cessation
#13
Jason D Robinson, Paul M Cinciripini, Maher Karam-Hage, Henri-Jean Aubin, Lowell C Dale, Raymond Niaura, Robert M Anthenelli
Despite the withdrawal of CB1 antagonists, such as rimonabant, from the market and from active clinical development because of concerns about their side effect profiles, research suggests that the endocannabinoid system may play an important role in modulating nicotine's effects. We report the combined results, using a pooled analysis, of three previously unpublished trials assessing rimonabant as a smoking cessation pharmacotherapy conducted between 2002 and 2004. Smokers (n = 2097) motivated to quit were enrolled in three randomized, double-blind, placebo-controlled trials, STRATUS EU, US, and META, which consisted of a 10-week treatment period with either rimonabant 20 mg (n = 789), 5 mg (n = 518; used in only two of the three studies), or placebo (n = 790), in conjunction with brief counseling...
April 21, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28429679/mycobacterium-avium-complex-disease
#14
Charles L Daley
Despite the ubiqitous nature of Mycobacterium avium complex (MAC) organisms in the environment, relatively few of those who are infected develop disease. Thus, some degree of susceptibility due to either underlying lung disease or immunosuppression is required. The frequency of pulmonary MAC disease is increasing in many areas, and the exact reasons are unknown. Isolation of MAC from a respiratory specimen does not necessarily mean that treatment is required, as the decision to treatment requires the synthesis of clinical, radiographic, and microbiologic information as well as a weighing of the risks and benefits for the individual patient...
April 2017: Microbiology Spectrum
https://www.readbyqxmd.com/read/28429631/household-food-insecurity-among-people-living-with-hiv-in-sagamu-nigeria-a-preliminary-study
#15
Oluwafolahan O Sholeye, Victor J Animasahun, Albert A Salako, Bankole K Oyewole
BACKGROUND: Household food insecurity has been associated with increased risk of transmission of HIV infection and poor treatment outcomes. This study therefore determined the prevalence of household food insecurity and its associated factors among people living with HIV in Sagamu, Ogun State, Nigeria. METHODS: A cross-sectional descriptive study was carried out among 244 adult clients accessing care and support at the teaching hospital in Sagamu, Nigeria, selected via systematic sampling...
January 1, 2017: Nutrition and Health
https://www.readbyqxmd.com/read/28429612/a-unique-database-for-gathering-data-from-a-mobile-app-and-medical-prescription-software-a-useful-data-source-to-collect-and-analyse-patient-reported-outcomes-of-depression-and-anxiety-symptoms
#16
Yoshinori Watanabe, Yoko Hirano, Yuko Asami, Maki Okada, Kazuya Fujita
A unique database named 'AN-SAPO' was developed by Iwato Corp. and Japan Brain Corp. in collaboration with the psychiatric clinics run by Himorogi Group in Japan. The AN-SAPO database includes patients' depression/anxiety score data from a mobile app named AN-SAPO and medical records from medical prescription software named 'ORCA'. On the mobile app, depression/anxiety severity can be evaluated by answering 20 brief questions and the scores are transferred to the AN-SAPO database together with the patients' medical records on ORCA...
April 21, 2017: International Journal of Psychiatry in Clinical Practice
https://www.readbyqxmd.com/read/28429554/is-there-a-practical-role-for-bone-biopsy-in-chronic-kidney-disease
#17
Terrence Diamond, Grahame J Elder
Bone biopsy is currently the only means to accurately assess renal osteodystrophy and responses to therapeutic interventions. With sedation, the technique is relatively painless, and complications are uncommon. Bone biopsy should be considered when the aetiology of symptoms or biochemical abnormalities is in question, and results may lead to changes in therapy. Although it remains prudent to use antiresorptive drugs cautiously in patients with chronic kidney disease (CKD) stages 3a-4 and low bone mineral density, bone biopsy may not be warranted before commencing therapy in these patients...
March 2017: Nephrology
https://www.readbyqxmd.com/read/28429411/nanodiscs-for-inpharma-nmr-characterization-of-gpcrs-ligand-binding-to-the-human-a2a-adenosine-receptor
#18
Kai Fredriksson, Philip Lottmann, Sonja Hinz, Iounut Onila, Aliaksei Shymanets, Christian Harteneck, Christa E Müller, Christian Griesinger, Thomas E Exner
G-protein-coupled-receptors (GPCRs) are of fundamental importance for signal transduction through cell membranes. This makes them important drug targets, but structure-based drug design (SBDD) is still hampered by the limitations for structure determination of unmodified GPCRs. We show that the interligand NOEs for pharmacophore mapping (INPHARMA) method can provide valuable information on ligand poses inside the binding site of the unmodified human A2A adenosine receptor reconstituted in nanodiscs. By comparing experimental INPHARMA spectra with back-calculated spectra based on ligand poses obtained from molecular dynamics simulations, a complex structure for A2A R with the low-affinity ligand 3-pyrrolidin-1-ylquinoxalin-2-amine was determined based on the X-ray structure of ligand ZM-241,358 in complex with a modified A2A R...
April 21, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28429378/expanding-access-to-naloxone-for-family-members-the-massachusetts-experience
#19
Sarah M Bagley, Leah S Forman, Sarah Ruiz, Kevin Cranston, Alexander Y Walley
INTRODUCTION AND AIMS: The Massachusetts Department of Public Health Overdose Education and Naloxone Distribution Program provides overdose education and naloxone rescue kits to people at risk for overdose and bystanders, including family members. Using Massachusetts Department of Public Health data, the aims are to: (i) describe characteristics of family members who receive naloxone; (ii) identify where family members obtain naloxone; and (iii) describe characteristics of rescues by family members...
April 20, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28429235/regulation-of-human-brain-microvascular-endothelial-cell-adhesion-and-barrier-functions-by-memantine
#20
Fei Wang, Zhirong Zou, Yi Gong, Dong Yuan, Xun Chen, Tao Sun
Vascular risk factors have been linked to cognitive decline and dementia in the elderly. Microvascular inflammation, especially of the endothelium, may contribute to the progression of neurodegenerative events in Alzheimer's disease (AD). Memantine, an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, is a licensed drug used for the treatment of moderate to severe AD. However, little information is available regarding its anti-inflammatory effects on the endothelium. In this study, we investigated the effects of memantine on human brain microvascular endothelial dysfunction induced by the pro-inflammatory cytokine tumor necrosis factor-α (TNF-α)...
April 20, 2017: Journal of Molecular Neuroscience: MN
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