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https://www.readbyqxmd.com/read/29471431/making-waves-new-developments-in-toxicology-with-the-zebrafish
#1
Katharine A Horzmann, Jennifer L Freeman
The laboratory zebrafish (Danio rerio) is now an accepted model in toxicologic research. The zebrafish model fills a niche between in vitro models and mammalian biomedical models. The developmental characteristics of the small fish are strategically being used by scientists to study topics ranging from high-throughput toxicity screens to toxicity in multi- and transgenerational studies. High-throughput technology has increased the utility of zebrafish embryonic toxicity assays in screening of chemicals and drugs for toxicity or effect...
February 19, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29470693/anti-inflammatory-anti-rheumatic-and-analgesic-activities-of-2-5-mercapto-1-3-4-oxadiazol-2-yl-n-propylbenzenesulphonamide-mopbs-in-rodents
#2
Hina Rasheed, Ruqayya Afridi, Ashraf Ullah Khan, Muhammad Zia Ullah, Sidra Khalid, Ayesha Atiq, Humaira Kashif, Muhammad Naeem Ahmed, Yeong Shik Kim, Salman Khan
Chronic inflammation is pathologically associated with various clinical conditions such as rheumatoid arthritis. Several anti-inflammatory and analgesic drugs currently available in market presents a wide range of problems. Therefore, the current study was aimed to evaluate anti-inflammatory and analgesic activities of newly synthesized compound 2-(5-mercapto-1,3,4-oxadiazol-2-yl)-N-propylbenzenesulphonamide (MOPBS). Carrageenan and CFA-induced models were developed for evaluation of anti-inflammatory and analgesic activity...
February 22, 2018: Inflammopharmacology
https://www.readbyqxmd.com/read/29470642/real-world-switching-to-riociguat-management-and-practicalities-in-patients-with-pah-and-cteph
#3
Henning Gall, Jean-Luc Vachiéry, Nobuhiro Tanabe, Michael Halank, Mauricio Orozco-Levi, Lisa Mielniczuk, MiKyung Chang, Kai Vogtländer, Ekkehard Grünig
PURPOSE: A proportion of patients with pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH) do not achieve treatment goals or experience side effects on their current therapy. In such cases, switching patients to a new drug while discontinuing the first may be a viable and appropriate treatment option. CAPTURE was designed to investigate how physicians manage the switching of patients to riociguat in real-world clinical practice. Observations from the study were used to assess whether recommendations in the riociguat prescribing information are reflected in clinical practice...
February 22, 2018: Lung
https://www.readbyqxmd.com/read/29470550/the-pregnane-x-receptor-pxr-and-the-nuclear-receptor-corepressor-2-ncor2-modulate-cell-growth-in-head-and-neck-squamous-cell-carcinoma
#4
Juan Pablo Rigalli, Matthias Reichel, Tasmin Reuter, Guillermo Nicolás Tocchetti, Gerhard Dyckhoff, Christel Herold-Mende, Dirk Theile, Johanna Weiss
Head and neck squamous cell carcinoma (HNSCC) is the sixth most frequent cancer worldwide. The pregnane X receptor (PXR) is a nuclear receptor regulating several target genes associated with cancer malignancy. We here demonstrated a significant effect of PXR on HNSCC cell growth, as evidenced in PXR knock-down experiments. PXR transcriptional activity is more importantly regulated by the presence of coactivators and corepressors than by PXR protein expression. To date, there is scarce information on the regulation of PXR in HNSCC and on its role in the pathogenesis of this disease...
2018: PloS One
https://www.readbyqxmd.com/read/29470517/two-essential-thioredoxins-mediate-apicoplast-biogenesis-protein-import-and-gene-expression-in-toxoplasma-gondii
#5
Marco Biddau, Anne Bouchut, Jack Major, Tracy Saveria, Julie Tottey, Ojore Oka, Marcel van-Lith, Katherine Elizabeth Jennings, Jana Ovciarikova, Amy DeRocher, Boris Striepen, Ross Frederick Waller, Marilyn Parsons, Lilach Sheiner
Apicomplexan parasites are global killers, being the causative agents of diseases like toxoplasmosis and malaria. These parasites are known to be hypersensitive to redox imbalance, yet little is understood about the cellular roles of their various redox regulators. The apicoplast, an essential plastid organelle, is a verified apicomplexan drug target. Nuclear-encoded apicoplast proteins traffic through the ER and multiple apicoplast sub-compartments to their place of function. We propose that thioredoxins contribute to the control of protein trafficking and of protein function within these apicoplast compartments...
February 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29470514/profile-of-suicide-attempts-and-risk-factors-among-psychiatric-patients-a-case-control-study
#6
Meha Bhatt, Stefan Perera, Laura Zielinski, Rebecca B Eisen, Sharon Yeung, Wala El-Sheikh, Jane DeJesus, Sumathy Rangarajan, Heather Sholer, Elizabeth Iordan, Pam Mackie, Shofiqul Islam, Mahshid Dehghan, Lehana Thabane, Zainab Samaan
BACKGROUND: Suicidal behaviour remains challenging for clinicians to predict, with few established risk factors and warning signs among psychiatric patients. AIM: We aimed to describe characteristics and identify risk factors for suicide attempts among patients with psychiatric disorders. METHODS: Multivariable logistic regression analysis, adjusted for clinically important confounders, was employed to determine risk factors for suicide attempts within a psychiatric patient population...
2018: PloS One
https://www.readbyqxmd.com/read/29470291/recurrent-abdominal-pain-in-children-summary-evidence-from-3-systematic-reviews-of-treatment-effectiveness
#7
Rebecca A Abbott, Alice E Martin, Tamsin V Newlove-Delgado, Alison Bethel, Rebecca S Whear, Jo Thompson Coon, Stuart Logan
OBJECTIVES: Between 4% and 25% of school-aged children complain of recurrent abdominal pain (RAP) severe enough to interfere with their daily activities. METHODS: We carried out a systematic review of randomised controlled trials (RCTs) in eleven databases and 2 trials registries from inception to June 2016. An update search was run in November 2017. All screening was performed by 2 independent reviewers. Included studies were appraised using the Cochrane risk of bias tool and the evidence assessed using GRADE...
February 21, 2018: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/29470101/ebselen-reversibly-inhibits-human-glutamate-dehydrogenase-at-the-catalytic-site
#8
Yanhong Jin, Di Li, Shiying Lu, Han Zhao, Zhao Chen, Wei Hou, Benfang Helen Ruan
Human glutamate dehydrogenase (GDH) plays an important role in neurological diseases, tumor metabolism, and hyperinsulinism-hyperammonemia syndrome (HHS). However, there are very few inhibitors known for human GDH. Recently, Ebselen was reported to crosslink with Escherichia coli GDH at the active site cysteine residue (Cys321), but the sequence alignment showed that the corresponding residue is Ala329 in human GDH. To investigate whether Ebselen could be an inhibitor for human GDH, we cloned and expressed an N-terminal His-tagged human GDH in E...
February 22, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29469575/herbicidins-from-streptomyces-sp-cb01388-showing-anti-cryptosporidium-activity
#9
Jian-Jun Chen, Mostafa E Rateb, Melissa S Love, Zhengren Xu, Dong Yang, Xiangcheng Zhu, Yong Huang, Li-Xing Zhao, Yi Jiang, Yanwen Duan, Case W McNamara, Ben Shen
A high-content imaging assay was used to screen the fraction collection of the Natural Product Library at The Scripps Research Institute for inhibitors of Cryptosporidium parvum. A chemical investigation of one strain, Streptomyces sp. CB01388, resulted in the isolation of six herbicidins (1-6), one of which is new (herbicidin L, 1). Five of the six herbicidins (1-3, 5, 6) showed moderate inhibitory activity against C. parvum, with 1 and 6 comparable to the FDA-approved drug nitazoxanide, and 2-6 showed no toxicity to the host HCT-8 cells and human HEK293T and HepG2 cells...
February 22, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29469240/actual-versus-expected-doses-of-half-tablets-containing-prescribed-psychoactive-substances-a-systematic-review
#10
Jaqueline K Eserian, Márcia Lombardo, Jair R Chagas, José C F Galduróz
Objective: To assess through a systematic review of the literature if the practice of splitting tablets containing psychoactive/psychotropic medications for medical or economic reasons would result in the expected doses. Data Sources: A MEDLINE and PsycInfo comprehensive search of English-language publications from January 1999 to December 2015 was conducted using the terms describing tablet splitting (tablet splitting, split tablets, tablet subdivision, divided tablets, and half tablets) and psychoactive substances (psychoactive medicines, psychotropic medicines, antidepressants, anxiolytics, anticonvulsants, antipsychotics, and antiparkinsonian agents)...
February 8, 2018: Primary Care Companion to CNS Disorders
https://www.readbyqxmd.com/read/29469221/molecular-recognition-by-a-short-partial-peptide-of-adrenergic-receptor-bottom-up-approach
#11
Tsubasa Sekiguchi, Masato Tamura, Hikari Oba, Pierre Çarçarbal, Rolando Rafael Lozada-Garcia, Anne Zehnacker-Rentien, Gilles Grégoire, Shun-Ichi Ishiuchi, Masaaki Fujii
Receptor-neurotransmitter molecular recognition is key of neurotransmission. Although crystal structures of the receptors are known, the mechanism for recognition is not clear. At present, the trial-and-error approach is the only sure method to identify ligands (e.g. drugs) that trigger the receptor. Here, we report the ultraviolet and infrared spectra of complexes between a partial peptide SIVSF, the binding motif of a catechol ring in the adrenergic receptor, and various ligands. The ultraviolet spectra show that two isomers coexist in the complex of SIVSF with properly recognized ligands, such as protonated adrenaline (adrenalineH+)...
February 22, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29468960/the-discovery-of-antibacterial-natural-compound-based-on-peptide-deformylase
#12
Li Liang, Qianqian Zhou, Zhixiang Hao, Fanfan Wang, Yasheng Zhu, Qisi Lin, Jian Gao
BACKGROUND: In recent years, Staphylococcus aureus have developed resistance to medicines used for the treatment of human infections. Therefore, the search for antibacterial agents of high potency against Staphylococcus aureus is of great concern. Peptide deformylase (PDF), a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins, has been considered to be an important antibacterial drug target. OBJECTIVE: To discover novel antibacterial drugs based on Staphylococcus aureus peptide deformylase...
February 20, 2018: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/29468867/a-simple-and-sensitive-method-for-determination-of-protein-kinase-activity-based-on-surface-charge-change-of-peptide-modified-gold-nanoparticles-as-substrates
#13
Fang Yi, Xiangyi Huang, Jicun Ren
Protein tyrosine kinases play a pivotal role in intracellular signal transduction pathways and oncogenic transformation. It is necessary to develop a simple, cost-effective and sensitive kinase assay for study of protein kinases and discovery of kinase-target drugs. In this paper, we present a simple and sensitive method for homogeneous detection of protein kinase activity and screening of inhibitor by measuring surface charge change on the peptide-modified gold nanoparticles (GNPs) as kinase substrates. In this assay, Abl (Abelson murine leukemia viral oncogene) kinase was used as a model...
February 22, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29468684/re-evaluation-of-the-regulation-of-omeprazole-in-racehorses-an-evidence-based-approach
#14
M Viljanto, L Hillyer, P Hincks, C Pearce, S W Paine
Medication control and doping control have been established in horse racing to ensure the integrity of the sport and the welfare of the horses. This ensures that horses do not compete under the influence of any drugs, including omeprazole, a therapeutic medication used to treat equine gastric ulcer syndrome. In this study, pharmacokinetic data were produced in equine plasma and urine following an oral administration of 4 mg/kg of generic buffered formulation of omeprazole to six Thoroughbred horses in five daily doses to determine an appropriate screening limit and detection time in equine plasma and to assess whether the current detection time of 72 hr in equine urine would be applicable when an alternative omeprazole product is administered...
February 22, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29468602/time-series-disturbance-detection-for-hypothesis-free-signal-detection-in-longitudinal-observational-databases
#15
Ed Whalen, Manfred Hauben, Andrew Bate
INTRODUCTION: Signal detection remains a cornerstone activity of pharmacovigilance. Routine quantitative signal detection primarily focuses on screening of spontaneous reports. In striving to enhance quantitative signal detection capability further, other data streams are being considered for their potential contribution as sources of emerging signals, one of which is longitudinal observational databases, including electronic medical record (EMR) and transactional insurance claims databases...
February 21, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/29468433/merging-perspectives-genotype-directed-molecular-therapy-for-hereditary-diffuse-gastric-cancer-hdgc-and-e-cadherin-egfr-crosstalk
#16
Dandan Li, Winifred Lo, Udo Rudloff
Hereditary diffuse gastric cancer is a cancer predisposition syndrome associated with germline mutations of the E-cadherin gene (CDH1; NM_004360). Male CDH1 germline mutation carriers have by the age of 80 years an estimated 70% cumulative incidence of gastric cancer, females of 56% for gastric and of 42% for lobular breast cancer. Metastatic HDGC has a poor prognosis which is worse than for sporadic gastric cancer. To date, there have been no treatment options described tailored to this molecular subtype of gastric cancer...
February 22, 2018: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/29467930/identification-of-the-potential-crucial-genes-in-invasive-ductal-carcinoma-using-bioinformatics-analysis
#17
Chunguang Li, Liangtao Luo, Sheng Wei, Xiongbiao Wang
Invasive ductal carcinoma (IDC) is a common histological type of breast cancer. The aim of this study was to identify the potential crucial genes associated with IDC and to provide valid biological information for further investigations. The gene expression profiles of GSE10780 which contained 42 histologically normal breast tissues and 143 IDC tissues were downloaded from the GEO database. Functional and pathway enrichment analysis of differentially expressed genes (DEGs) were performed and protein-protein interaction (PPI) network was analyzed using Cytoscape...
January 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29467872/differential-microrna-expression-profiles-in-tamoxifen-resistant-human-breast-cancer-cell-lines-induced-by-two-methods
#18
Peng Ye, Cheng Fang, Hui Zeng, Yu Shi, Zhongya Pan, Nairui An, Keli He, Li Zhang, Xinghua Long
Tamoxifen (TAM) resistance has become a severe problem for endocrine therapy of breast cancer. The present study investigated the association between microRNA (miRNA) expression and TAM resistance in breast cancer. The TAM-resistant breast cancer MCF-7C and MCF-7T cell lines were established using the human breast cancer cell line MCF-7 as the parental cell line and 4-hydroxytamoxifen (OHT) as the screening drug in vitro . The MCF-7C cell line was established by dose stepwise induction beginning with a low concentration of OHT; the MCF-7T cell line was established by temporal stepwise induction beginning with a high concentration of OHT...
March 2018: Oncology Letters
https://www.readbyqxmd.com/read/29467650/additive-dose-response-models-explicit-formulation-and-the-loewe-additivity-consistency-condition
#19
Simone Lederer, Tjeerd M H Dijkstra, Tom Heskes
High-throughput techniques allow for massive screening of drug combinations. To find combinations that exhibit an interaction effect, one filters for promising compound combinations by comparing to a response without interaction. A common principle for no interaction is Loewe Additivity which is based on the assumption that no compound interacts with itself and that two doses from different compounds having the same effect are equivalent. It then should not matter whether a component is replaced by the other or vice versa...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29467610/open-science-meets-stem-cells-a-new-drug-discovery-approach-for-neurodegenerative-disorders
#20
REVIEW
Chanshuai Han, Mathilde Chaineau, Carol X-Q Chen, Lenore K Beitel, Thomas M Durcan
Neurodegenerative diseases are a challenge for drug discovery, as the biological mechanisms are complex and poorly understood, with a paucity of models that faithfully recapitulate these disorders. Recent advances in stem cell technology have provided a paradigm shift, providing researchers with tools to generate human induced pluripotent stem cells (iPSCs) from patient cells. With the potential to generate any human cell type, we can now generate human neurons and develop "first-of-their-kind" disease-relevant assays for small molecule screening...
2018: Frontiers in Neuroscience
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