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https://www.readbyqxmd.com/read/27926729/intracellular-allosteric-antagonism-of-the-ccr9-receptor
#1
Christine Oswald, Mathieu Rappas, James Kean, Andrew S Doré, James C Errey, Kirstie Bennett, Francesca Deflorian, John A Christopher, Ali Jazayeri, Jonathan S Mason, Miles Congreve, Robert M Cooke, Fiona H Marshall
Chemokines and their G-protein-coupled receptors play a diverse role in immune defence by controlling the migration, activation and survival of immune cells. They are also involved in viral entry, tumour growth and metastasis and hence are important drug targets in a wide range of diseases. Despite very significant efforts by the pharmaceutical industry to develop drugs, with over 50 small-molecule drugs directed at the family entering clinical development, only two compounds have reached the market: maraviroc (CCR5) for HIV infection and plerixafor (CXCR4) for stem-cell mobilization...
December 7, 2016: Nature
https://www.readbyqxmd.com/read/27925499/non-adherence-to-psychotropic-medication-among-adolescents-a-systematic-review-of-the-literature
#2
Alexander Häge, Lisa Weymann, Lucia Bliznak, Viktoria Märker, Konstantin Mechler, Ralf W Dittmann
INTRODUCTION: Whether patients take their medication as prescribed is of increasing importance in adolescent psychiatry since both the number of efficacious pharmaceutical treatments and the rate of prescriptions of psychotropic compounds are on the rise. Previous research showed high rates of medication nonadherence among both adolescents with medical disorders and adult patients with psychiatric disorders. METHODS: The present review was performed according to PRISMA guidelines and evaluates existing scientific literature concerning adherence to psychotropic medication among adolescents...
December 7, 2016: Zeitschrift Für Kinder- und Jugendpsychiatrie und Psychotherapie
https://www.readbyqxmd.com/read/27925269/lifecycle-exposure-of-fathead-minnows-to-environmentally-relevant-concentrations-of-the-%C3%AE-blocker-drug-propranolol
#3
Joanne L Parrott, Vimal K Balakrishnan
Propranolol is a human pharmaceutical β-blocker that has been detected in municipal wastewater effluents at ng/L to low µg/L. To assess the potential of this compound to affect fish, fathead minnow (Pimephales promelas) were exposed for a lifecycle in a flow-through system to nominal propranolol concentrations of 0.87, 8.7, 87, 870 and 8,700 ng/L. Measured propranolol concentrations were below detection for the two lowest exposure concentrations, and were 76, 580, and 7,800 ng/L for the three highest exposure concentrations...
December 7, 2016: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/27924981/hts-ftir-spectroscopy-allows-the-classification-of-polyphenols-according-to-their-differential-effects-on-the-mda-mb-231-breast-cancer-cell-line
#4
A Mignolet, V Mathieu, E Goormaghtigh
Breast cancer is a major public health issue among women in the world. Meanwhile new anticancer treatments struggle more and more to be accepted in the pharmaceutical market and research costs still increase. There is therefore a need to find new treatments and new screening methods to test them more quickly and efficiently. Among natural compounds, an increasing interest has been given to polyphenols as they can take action at the different stages of carcinogenesis, from tumour initiation to metastasis formation, by disturbing multiple cellular signalling pathways...
December 7, 2016: Analyst
https://www.readbyqxmd.com/read/27924725/anticancer-drug-targets-of-salvia-phytometabolites-chemistry-biology-and-omics
#5
Da-Cheng Hao, Guang-Bo Ge, Pei-Gen Xiao
Salvia displays diverse anticancer properties, which are attributable to their diterpene and phenolic contents. There is no comprehensive review on the anticancer diversity and molecular targets of Salvia components. We investigate the diversity and molecular targets of Salvia phytometabolites responsible for the prevention and treatment of cancer and sarcoma. Traditional therapeutic knowledge suggests that Salvia species can be used to develop anticancer drugs. Lots of concerns have been raised for tanshinone (Tan) IIA and cryptotanshinone...
December 7, 2016: Current Drug Targets
https://www.readbyqxmd.com/read/27924551/mycotoxins-a-fungal-genomics-perspective
#6
Daren W Brown, Scott E Baker
The chemical and enzymatic diversity in the fungal kingdom is staggering. Large-scale fungal genome sequencing projects are generating a massive catalog of secondary metabolite biosynthetic genes and pathways. Fungal natural products are a boon and bane to man as valuable pharmaceuticals and harmful toxins. Understanding how these chemicals are synthesized will aid the development of new strategies to limit mycotoxin contamination of food and feeds as well as expand drug discovery programs. A survey of work focused on the fumonisin family of mycotoxins highlights technological advances and provides a blueprint for future studies of other fungal natural products...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27924323/the-use-of-a-quartz-crystal-microbalance-as-an-analytical-tool-to-monitor-particle-surface-and-particle-particle-interactions-under-dry-ambient-and-pressurized-conditions-a-study-using-common-inhaler-components
#7
N W Turner, M Bloxham, S A Piletsky, M J Whitcombe, I Chianella
Metered dose inhalers (MDI) and multidose powder inhalers (MPDI) are commonly used for the treatment of chronic obstructive pulmonary diseases and asthma. Currently, analytical tools to monitor particle/particle and particle/surface interaction within MDI and MPDI at the macro-scale do not exist. A simple tool capable of measuring such interactions would ultimately enable quality control of MDI and MDPI, producing remarkable benefits for the pharmaceutical industry and the users of inhalers. In this paper, we have investigated whether a quartz crystal microbalance (QCM) could become such a tool...
December 7, 2016: Analyst
https://www.readbyqxmd.com/read/27924120/hippophae-rhamnoides-n-glycoproteome-analysis-a-small-step-towards-sea-buckthorn-proteome-mining
#8
Yaiphabi Sougrakpam, Renu Deswal
Hippophae rhamnoides is a hardy shrub capable of growing under extreme environmental conditions namely, high salt, drought and cold. Its ability to grow under extreme conditions and its wide application in pharmaceutical and nutraceutical industry calls for its in-depth analysis. N-glycoproteome mining by con A affinity chromatography from seedling was attempted. The glycoproteome was resolved on first and second dimension gel electrophoresis. A total of 48 spots were detected and 10 non-redundant proteins were identified by MALDI-TOF/TOF...
October 2016: Physiology and Molecular Biology of Plants: An International Journal of Functional Plant Biology
https://www.readbyqxmd.com/read/27923949/novel-bumped-kinase-inhibitors-are-safe-and-effective-therapeutics-in-the-calf-clinical-model-for-cryptosporidiosis
#9
Deborah A Schaefer, Dana P Betzer, Kylie D Smith, Zachary G Millman, Hannah C Michalski, Sarah E Menchaca, Jennifer A Zambriski, Kayode K Ojo, Matthew A Hulverson, Samuel L M Arnold, Kasey L Rivas, Rama S R Vidadala, Wenlin Huang, Lynn K Barrett, Dustin J Maly, Erkang Fan, Wesley C Van Voorhis, Michael W Riggs
Cryptosporidiosis, caused by the apicomplexan parasite Cryptosporidium parvum, is a diarrheal disease that has produced a large global burden in mortality and morbidity in humans and livestock. There are currently no consistently effective parasite-specific pharmaceuticals available for this disease. Bumped kinase inhibitors (BKIs) specific for parasite calcium-dependent protein kinases (CDPKs) have been shown to reduce infection in several parasites having medical and veterinary importance, including Toxoplasma gondii, Plasmodium falciparum, and C...
December 15, 2016: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/27923696/correlating-gastric-emptying-of-amphotericin-b-and-paracetamol-solid-lipid-nanoparticles-with-changes-in-particle-surface-chemistry
#10
Hilda Amekyeh, Nashiru Billa, Clive Roberts
Oral delivery of pharmaceuticals requires that they retain their physical and chemical attributes during transit within the gastrointestinal (GI) tract, for the manifestation of desired therapeutic profiles. Solid lipid nanoparticles (SLNs) are used as carriers to improve the absorption of hydrophobic drugs. In this study, we examine the stability of amphotericin B (AmB) and paracetamol (PAR) SLNs in simulated GI fluids during gastric emptying. On contact with the simulated fluids, the particles increased in size due to ingress of the dissolution media into the particles...
December 3, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27923198/detoxification-with-titration-and-tapering-in-gamma-hydroxybutyrate-ghb-dependent-patients-the-dutch-ghb-monitor-project
#11
Boukje A G Dijkstra, Rama Kamal, Martijn S van Noorden, Hein de Haan, Anton J M Loonen, Cor A J De Jong
BACKGROUND AND AIMS: Gamma-hydroxybutyrate (GHB) detoxification procedures have been insufficiently studied for effectiveness and safety. Based on case reports, benzodiazepines are generally regarded as first-choice agents in GHB detoxification. Detoxification by titration and tapering (DeTiTap) with pharmaceutical GHB in an open-label consecutive case series of 23 GHB-dependent patients showed to be feasible, effective and safe. This study further explored the feasibility, effectiveness and safety of this detoxification procedure in a large group of patients...
November 21, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/27923138/metallogel-templated-synthesis-and-stabilization-of-silver-particles-and-its-application-in-catalytic-reduction-of-nitro-arene
#12
Mukesh Sharma, Plaban Jyoti Sarma, Manash Jyoti Goswami, Kusum K Bania
Metallogel of iron-carboxylates was obtained from trans-1,2-cyclohexanedicarboxylic acid in dimethylformamide (DMF) at basic condition. Spectroscopic and SEM morphology study of the iron-metallogel revealed that the iron complex with dicarboxylic acid was linked together via carboxylates and led to a supramolecular helical like architecture. The synthesized metallogel served as an excellent template for in-situ reduction of silver ion to silver particles micro to nano scale range. Variation of AgNO3 concentration shepherd to change the morphology of the Ag-particles...
November 20, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27922739/tyrosine-kinase-aurora-kinase-and-leucine-aminopeptidase-as-attractive-drug-targets-in-anticancer-therapy-characterisation-of-their-inhibitors
#13
Joanna Ziemska, Jolanta Solecka
Cancers are the leading cause of deaths all over the world. Available anticancer agents used in clinics exhibit low therapeutic index and usually high toxicity. Wide spreading drug resistance of cancer cells induce a demanding need to search for new drug targets. Currently, many on-going studies on novel compounds with potent anticancer activity, high selectivity as well as new modes of action are conducted. In this work, we describe in details three enzyme groups, which are at present of extensive interest to medical researchers and pharmaceutical companies...
2016: Roczniki Państwowego Zakładu Higieny
https://www.readbyqxmd.com/read/27922722/topiramate-versus-carbamazepine-monotherapy-for-epilepsy-an-individual-participant-data-review
#14
REVIEW
Sarah J Nolan, Maria Sudell, Catrin Tudur Smith, Anthony G Marson
BACKGROUND: Epilepsy is a common neurological condition in which abnormal electrical discharges from the brain cause recurrent unprovoked seizures. It is believed that with effective drug treatment, up to 70% of individuals with active epilepsy have the potential to become seizure-free and go into long-term remission shortly after starting drug therapy, the majority of which may be able to achieve remission with a single antiepileptic drug (AED).The correct choice of first-line antiepileptic therapy for individuals with newly diagnosed seizures is of great importance...
December 6, 2016: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/27922200/a-fluorescence-lifetime-based-binding-assay-for-class-iia-histone-deacetylases
#15
Christian Meyners, Monique Mertens, Pablo Wessig, Franz-Josef Meyer-Almes
Class IIa HDACs show extremely low enzymatic activity and no commonly accepted endogenous substrate is known today. Increasing evidence suggests that these enzymes exert their effect rather through molecular recognition of acetylated proteins and recruiting other proteins like HDAC3 to the desired target location. Accordingly, class IIa HDACs like bromodomains have been suggested to act as "Readers" of acetyl marks, whereas enzymatically active HDACs from class I or IIb are called "Erasers" to highlight their capability to remove acetyl groups from acetylated histones or other proteins...
December 6, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27922103/hypothalamic-activation-is-essential-for-endotoxemia-induced-acute-muscle-wasting
#16
Kaipeng Duan, Qiyi Chen, Minhua Cheng, Chenyan Zhao, Zhiliang Lin, Shanjun Tan, Fengchan Xi, Tao Gao, Jialiang Shi, Juanhong Shen, Weiqin Li, Wenkui Yu, Jieshou Li, Ning Li
Growing evidence suggests acute skeletal muscle wasting is a key factor affecting nutritional support and prognosis in critical patients. Previously, plenty of studies of muscle wasting focused on the peripheral pathway, little was known about the central role. We tested the hypothesis whether central inflammatory pathway and neuropeptides were involved in the process. In lipopolysaccharide (LPS) treated rats, hypothalamic NF-κB pathway and inflammation were highly activated, which was accompanied with severe muscle wasting...
December 6, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27922016/gabaergic-anxiolytic-drug-in-water-increases-migration-behaviour-in-salmon
#17
Gustav Hellström, Jonatan Klaminder, Fia Finn, Lo Persson, Anders Alanärä, Micael Jonsson, Jerker Fick, Tomas Brodin
Migration is an important life-history event in a wide range of taxa, yet many migrations are influenced by anthropogenic change. Although migration dynamics are extensively studied, the potential effects of environmental contaminants on migratory physiology are poorly understood. In this study we show that an anxiolytic drug in water can promote downward migratory behaviour of Atlantic salmon (Salmo salar) in both laboratory setting and in a natural river tributary. Exposing salmon smolt to a dilute concentration of a GABAA receptor agonist (oxazepam) increased migration intensity compared with untreated smolt...
December 6, 2016: Nature Communications
https://www.readbyqxmd.com/read/27921450/oral-pharmacokinetic-interaction-of-ester-rich-fruit-juices-and-pharmaceutical-excipients-with-tenofovir-disoproxil-fumarate-in-male-wistar-rats
#18
Joseph Shailender, Punna Rao Ravi, Paramita Saha, Srividya Myneni
The aim of this study was to evaluate the role of intestinal esterases on the absorption process of tenofovir disoproxil fumarate (TDF). The esterase inhibition capacity of fruit juices (FJs) rich in ester linkages and pharmaceutical excipients (having ester) was performed in vitro by incubating TDF with each FJ and excipient in the intestinal washings. The ex vivo everted gut sac model was also used to evaluate the absorption enhancement capacity of these FJs and excipients. Single dose oral pharmacokinetic studies were performed by concomitant administration of TDF with each of the selected FJs and excipients...
December 6, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27921310/chiral-selectors-in-ce-recent-development-and-applications-mid-2014-mid-2016
#19
REVIEW
Ioannis J Stavrou, Eliana A Agathokleous, Constantina P Kapnissi-Christodoulou
This report, which is a sequence of a series of reviews, records the most important chiral selectors (CSs) applied in CE. It highlights the CSs that were used during the period 2014 to mid 2016. In this review, method developments, validations, and pharmaceutical along with biomedical applications are presented. The different CSs include cyclodextrins, antibiotics, cyclofructants, linear and branched oligo- and polysaccharides and polymeric surfactants. In addition, the advantages of these CSs, along with their chiral recognition mechanisms, and their performance, are discussed...
December 6, 2016: Electrophoresis
https://www.readbyqxmd.com/read/27921147/can-the-alendronate-dosage-be-altered-when-combined-with-high-frequency-loading-in-osteoporosis-treatment
#20
C B Correa, G V Camargos, M Chatterjee, M F Mesquita, A A Del Bel Cury, I Naert, J Duyck, K Vandamme
: Alendronate therapy has been associated with serious side effects. Altering the alendronate concentration and combining with high-frequency loading as mechanical intervention was explored in this animal study as a treatment for osteoporosis. The bone anabolic potency of high-frequency loading was overruled by the different alendronate dosages applied in the present study. Further exploration of reduced hormonal therapy associated with mechanical interventions in osteoporosis treatment should be sought...
December 5, 2016: Osteoporosis International
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