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https://www.readbyqxmd.com/read/28550735/clarithromycin-inhibits-tnf-%C3%AE-induced-muc5ac-mucin-gene-expression-via-the-mkp-1-p38mapk-dependent-pathway
#1
Said Ahmad Shah, Hajime Ishinaga, Kazuhiko Takeuchi
Clarithromycin is a 14-membered macrolide antibiotic. Low-dose, long-term macrolide therapy is effective in patients with chronic airway diseases, such as diffuse panbronchitis, chronic bronchitis, and chronic sinusitis. However, the mechanism underlying this clinical efficacy remains unclear. The dual specificity phosphatase MKP-1 (MAPK phosphatase-1), also called DUSP (dual specificity phosphatase-1), was initially identified as an in vitro ERK-specific phosphatase, but depending on the cell type, it can also dephosphorylate other members of the MAPK family, such as p38 and JNK, and thus suppress downstream signaling of these kinases...
May 24, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28550637/breaking-bad-the-structure-and-function-of-the-blood-brain-barrier-in-epilepsy
#2
Hadas Han, Aniv Mann, Dana Ekstein, Sara Eyal
Epilepsy is a neurological disease with variable etiology and clinical manifestation, affecting more than 50 million people worldwide. Although the ultimate precipitators of seizures are neurons, it is becoming evident that epileptic activity is associated with changes in the function of other cell types, including those consisting the blood-brain barrier (BBB) and regulating its permeability. The interrelationships between impaired BBB function and epilepsy are complex, as BBB dysfunction may both lead to seizures and be induced by epileptic activity...
May 26, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28550609/validation-of-the-taps-1-a-four-item-screening-tool-to-identify-unhealthy-substance-use-in-primary-care
#3
Jan Gryczynski, Jennifer McNeely, Li-Tzy Wu, Geetha A Subramaniam, Dace S Svikis, Lauretta A Cathers, Gaurav Sharma, Jacqueline King, Eve Jelstrom, Courtney D Nordeck, Anjalee Sharma, Shannon G Mitchell, Kevin E O'Grady, Robert P Schwartz
BACKGROUND: The Tobacco, Alcohol, Prescription Medication, and Other Substance use (TAPS) tool is a combined two-part screening and brief assessment developed for adult primary care patients. The tool's first-stage screening component (TAPS-1) consists of four items asking about past 12-month use for four substance categories, with response options of never, less than monthly, monthly, weekly, and daily or almost daily. OBJECTIVE: To validate the TAPS-1 in primary care patients...
May 26, 2017: Journal of General Internal Medicine
https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#4
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28550595/clinical-pharmacokinetics-and-pharmacodynamics-of-colistin
#5
REVIEW
Nicolas Grégoire, Vincent Aranzana-Climent, Sophie Magréault, Sandrine Marchand, William Couet
In this review, we provide an updated summary on colistin pharmacokinetics and pharmacodynamics. Colistin is an old molecule that is frequently used as last-line treatment for infections caused by multidrug-resistant Gram-negative bacteria. Colistin is a decapeptide administered either as a prodrug, colistin methanesulfonate (CMS), when used intravenously, or as colistin sulfate when used orally. Because colistin binds to laboratory materials, many experimental issues are raised and studies on colistin can be tricky...
May 26, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28550519/drug-abuse-associated-mortality-across-the-lifespan-a-population-based-longitudinal-cohort-and-co-relative-analysis
#6
Kenneth S Kendler, Henrik Ohlsson, Kristina Sundquist, Jan Sundquist
PURPOSE: Nationwide data have been lacking on drug abuse (DA)-associated mortality. We do not know the degree to which this excess mortality results from the characteristics of drug-abusing individuals or from the effects of DA itself. METHOD: DA was assessed from medical, criminal, and prescribed drug registries. Relative pairs discordant for DA were obtained from the Multi-Generation and Twin Registers. Mortality was obtained from the Swedish Mortality registry...
May 26, 2017: Social Psychiatry and Psychiatric Epidemiology
https://www.readbyqxmd.com/read/28550480/characteristics-associated-with-quality-of-life-among-people-with-drug-resistant-epilepsy
#7
Leone Ridsdale, Gabriella Wojewodka, Emily Robinson, Sabine Landau, Adam Noble, Stephanie Taylor, Mark Richardson, Gus Baker, Laura H Goldstein
Quality of Life (QoL) is the preferred outcome in non-pharmacological trials, but there is little UK population evidence of QoL in epilepsy. In advance of evaluating an epilepsy self-management course we aimed to describe, among UK participants, what clinical and psycho-social characteristics are associated with QoL. We recruited 404 adults attending specialist clinics, with at least two seizures in the prior year and measured their self-reported seizure frequency, co-morbidity, psychological distress, social characteristics, including self-mastery and stigma, and epilepsy-specific QoL (QOLIE-31-P)...
May 26, 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28550457/treatment-of-juvenile-dermatomyositis-an-update
#8
REVIEW
Charalampia Papadopoulou, Lucy R Wedderburn
The idiopathic inflammatory myopathies of childhood consist of a heterogeneous group of autoimmune diseases characterised by proximal muscle weakness and pathognomonic skin rashes. The overall prognosis of juvenile myositis has improved significantly over recent years, but the long-term outcome differs substantially from patient to patient, suggestive of distinct clinical phenotypes with variable responses to treatment. High doses of corticosteroids remain the cornerstone of therapy along with other immunosuppressant therapies depending on disease severity and response...
May 26, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28550447/trends-in-surgical-research-in-head-and-neck-cancer
#9
REVIEW
Genrich Tolstonog, Christian Simon
The task of surgical research is to improve the efficacy of available surgical therapeutic modalities, develop new ones, and balance this well with favorable functional outcome. Therefore, surgical research is composed of a translational and a clinical component. In translational surgical research, animal models are used to better understand the biology of head and neck cancers, but even more importantly, the biology of changes to the disease and the microenvironment created by surgical interventions. Animal models additionally allow for the development of image-guided surgery systems, novel strategies of intraoperative adjuvant treatment, and patient "avatars" to test innovative anticancer drug combinations...
June 2017: Current Treatment Options in Oncology
https://www.readbyqxmd.com/read/28550360/bioprinting-technologies-for-disease-modeling
#10
REVIEW
Adnan Memic, Ali Navaei, Bahram Mirani, Julio Alvin Vacacela Cordova, Musab Aldhahri, Alireza Dolatshahi-Pirouz, Mohsen Akbari, Mehdi Nikkhah
There is a great need for the development of biomimetic human tissue models that allow elucidation of the pathophysiological conditions involved in disease initiation and progression. Conventional two-dimensional (2D) in vitro assays and animal models have been unable to fully recapitulate the critical characteristics of human physiology. Alternatively, three-dimensional (3D) tissue models are often developed in a low-throughput manner and lack crucial native-like architecture. The recent emergence of bioprinting technologies has enabled creating 3D tissue models that address the critical challenges of conventional in vitro assays through the development of custom bioinks and patient derived cells coupled with well-defined arrangements of biomaterials...
May 26, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28550305/dynamics-and-ligand-induced-conformational-changes-in-human-prolyl-oligopeptidase-analyzed-by-hydrogen-deuterium-exchange-mass-spectrometry
#11
Alexandra Tsirigotaki, Roos Van Elzen, Pieter Van Der Veken, Anne-Marie Lambeir, Anastassios Economou
Prolyl oligopeptidase (PREP) is conserved in many organisms across life. It is involved in numerous processes including brain function and neuropathology, that require more than its strict proteolytic role. It consists of a seven-bladed β-propeller juxtaposed to a catalytic α/β-hydrolase domain. The conformational dynamics of PREP involved in domain motions and the gating mechanism that allows substrate accessibility remain elusive. Here we used Hydrogen Deuterium eXchange Mass Spectrometry (HDX-MS) to derive the first near-residue resolution analysis of global PREP dynamics in the presence or absence of inhibitor bound in the active site...
May 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28550094/safety-of-outpatient-initiation-of-disopyramide-for-obstructive-hypertrophic-cardiomyopathy-patients
#12
Arnon Adler, Dana Fourey, Adaya Weissler-Snir, Waseem Hindieh, Raymond H Chan, Michael H Gollob, Harry Rakowski
BACKGROUND: Disopyramide is effective in ameliorating symptoms in patients with hypertrophic cardiomyopathy; however, its potential for proarrhythmic effect has raised concerns about its use in the ambulatory setting. The risk of initiating disopyramide in this manner has never been evaluated. METHODS AND RESULTS: All charts of patients seen in the outpatient hypertrophic cardiomyopathy clinic between 2010 and 2014 were screened for initiation of disopyramide and data were extracted...
May 26, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28550055/potential-drug-interactions-mediated-by-renal-organic-anion-transporter-oatp4c1
#13
Toshihiro Sato, Eikan Mishima, Nariyasu Mano, Takaaki Abe, Hiroaki Yamaguchi
OATP4C1 is an organic anion transporter expressed in the basolateral membrane of the renal proximal tubules. It plays a major role in the urinary excretion of both exogenous drugs and endogenous compounds. Our previous studies have indicated the importance of OATP4C1 in pathological and physiological conditions; however, the majority of its pharmacological characteristics remained unclear. Therefore, to provide essential information for clinical drug therapy decisions and drug development, we, in this study, attempted to clarify drug interactions mediated by OATP4C1...
May 26, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28550040/kras-g12d-expression-in-lung-resident-myeloid-cells-promotes-pulmonary-lch-like-neoplasm-sensitive-to-statin-treatment
#14
Tamihiro Kamata, Susan Giblett, Catrin Pritchard
Langerhans cell histiocytosis (LCH) is a rare histiocytic neoplasm associated with somatic mutations in the genes involved in the RAF/MEK/ERK signaling pathway. Recently, oncogenic mutations in NRAS/KRAS, upstream regulators of the RAF/MEK/ERK pathway, have been reported in pulmonary, but not in non-pulmonary, LCH cases, suggesting organ-specific contribution of oncogenic RAS to LCH pathogenesis. Using a mouse model expressing KRAS(G12D) in the lung by nasal delivery of adenoviral Cre, here we show that KRAS(G12D) expression in lung-resident myeloid cells induces pulmonary LCH-like neoplasms comprised of pathogenic CD11c(high)F4/80+CD207+ cells...
May 26, 2017: Blood
https://www.readbyqxmd.com/read/28549907/transformation-of-bcs-class-i-and-iii-drugs-into-ionic-liquids-and-lipophilic-salts-for-enhanced-developability-using-lipid-formulations
#15
Hywel D Williams, Leigh Ford, Shea Lim, Sifei Han, John Baumann, Hannah Sullivan, David Vodak, Annabel Igonin, Hassan Benameur, Colin W Pouton, Peter J Scammells, Christopher J H Porter
Higher lipid solubility of lipophilic salt forms creates new product development opportunities for high-dose liquid-filled capsules. The purpose of this study was to determine if lipophilic salts of BCS Class I amlodipine and BCS Class III fexofenadine, ranitidine and metformin were better lipid formulation candidates than existing commercial salts. Lipophilic salts were prepared from lipophilic anions and commercial HCl or besylate salt forms, as verified by (1)H NMR. Thermal properties were assessed by DSC and hot-stage microscopy...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549889/synthesis-and-evaluation-of-novel-dual-brd4-hdac-inhibitors
#16
Seika Amemiya, Takao Yamaguchi, Yuichi Hashimoto, Tomomi Noguchi-Yachide
Epigenetic regulation of gene expression via histone acetylation modulates many cellular processes, including apoptosis, the cell cycle, cell growth and differentiation, and inhibitors are promising drug candidates. We have previously developed inhibitors of BRD4, which recognizes acetylated lysine residue on histones and recruits transcription elongation factor to the transcription start site, while inhibitors of histone deacetylase (HDAC), which catalyzes the removal of acetyl groups on histones, are already in clinical use for cancer treatment...
May 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549888/synthesis-of-n%C3%AE-vel-artemisinin-dimers-with-polyamine-linkers-and-evaluation-of-their-potential-as-anticancer-agents
#17
George E Magoulas, Tzoanna Tsigkou, Lina Skondra, Margarita Lamprou, Panagiota Tsoukala, Vassiliki Kokkinogouli, Evangelia Pantazaka, Dionissios Papaioannou, Constantinos M Athanassopoulos, Evangelia Papadimitriou
The natural product artemisinin and derivatives thereof are currently considered as the drugs of choice for the treatment of malaria. At the same time, a significant number of such drugs have also shown interesting anticancer activity. In the context of the present research work, artemisinin was structurally modified and anchored to naturally occurring polyamines to afford new artemisinin dimeric conjugates whose potential anticancer activity was evaluated. All artemisinin conjugates tested were more effective than artemisinin itself in decreasing the number of MCF7 breast cancer cells...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549824/the-hsp90-chaperone-network-modulates-candida-virulence-traits
#18
REVIEW
Teresa R O'Meara, Nicole Robbins, Leah E Cowen
Hsp90 is a conserved molecular chaperone that facilitates the folding and function of client proteins. Hsp90 function is dynamically regulated by interactions with co-chaperones and by post-translational modifications. In the fungal pathogen Candida albicans, Hsp90 enables drug resistance and virulence by stabilizing diverse signal transducers. Here, we review studies that have unveiled regulators of Hsp90 function, as well as downstream effectors that govern the key virulence traits of morphogenesis and drug resistance...
May 23, 2017: Trends in Microbiology
https://www.readbyqxmd.com/read/28549799/a-randomized-controlled-trial-of-the-impact-of-pharmacist-led-patient-centered-pharmaceutical-care-on-patients-medicine-therapy-related-quality-of-life
#19
Phantipa Sakthong, Todsaporn Sangthonganotai
BACKGROUND: Due to a lack of pharmaceutical care (PC)-specific measures for health-related quality of life, a novel generic questionnaire "Patient-Reported Outcomes Measure of Pharmaceutical Therapy for Quality of Life (PROMPT-QoL) was developed. Little was also known about an impact of pharmaceutical care on medicine therapy-related quality of life. OBJECTIVE: First, evaluate the impact of PC on medicine therapy-related QoL using the PROMPT-QoL in Thai patients...
May 11, 2017: Research in Social & Administrative Pharmacy: RSAP
https://www.readbyqxmd.com/read/28549786/action-potential-based-mea-platform-for-in-vitro-screening-of-drug-induced-cardiotoxicity-using-human-ipscs-and-rat-neonatal-myocytes
#20
Danny Jans, Geert Callewaert, Olga Krylychkina, Luis Hoffman, Francesco Gullo, Dimiter Prodanov, Dries Braeken
Drug-induced cardiotoxicity poses a negative impact on public health and drug development. Cardiac safety pharmacology issues urged for the preclinical assessment of drug-induced ventricular arrhythmia leading to the design of several in vitro electrophysiological screening assays. In general, patch clamp systems allow for intracellular recordings, while multi-electrode array (MEA) technology detect extracellular activity. Here, we demonstrate a complementary metal oxide semiconductor (CMOS)-based MEA system as a reliable platform for non-invasive, long-term intracellular recording of cardiac action potentials at high resolution...
May 23, 2017: Journal of Pharmacological and Toxicological Methods
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