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Assay and Drug Development Technologies

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https://www.readbyqxmd.com/read/29215913/high-content-screening-comparison-of-cancer-drug-accumulation-and-distribution-in-two-dimensional-and-three-dimensional-culture-models-of-head-and-neck-cancer
#1
Feng Shan, David A Close, Daniel P Camarco, Paul A Johnston
High cancer drug development attrition rates have provoked considerable debate about whether the two-dimensional tumor growth inhibition high-throughput screening assays used in pre-clinical lead discovery adequately reflect solid tumor complexity. We used automated high-content screening image acquisition and analysis methods to compare fluorescent drug uptake, accumulation, and distribution in Cal33 and FaDu head and neck cancer (HNC) monolayer and multicellular tumor spheroid (MCTS) models. Ellipticine, idarubicin, daunorubicin, and doxorubicin were studied because of their fluorescent properties and broad anti-tumor activities...
December 7, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29193979/when-enough-is-enough-decision-criteria-for-moving-a-known-drug-into-clinical-testing-for-a-new-indication-in-the-absence-of-preclinical-efficacy-data
#2
Jill M Pulley, Rebecca N Jerome, Nicole M Zaleski, Jana K Shirey-Rice, Andrea J Pruijssers, Robert R Lavieri, Somsundaram N Chettiar, Helen M Naylor, David M Aronoff, David A Edwards, Colleen M Niswender, Laura L Dugan, Leslie J Crofford, Gordon R Bernard, Kenneth J Holroyd
Many animal models of disease are suboptimal in their representation of human diseases and lack of predictive power in the success of pivotal human trials. In the context of repurposing drugs with known human safety, it is sometimes appropriate to conduct the "last experiment first," that is, progressing directly to human investigations. However, there are not accepted criteria for when to proceed straight to humans to test a new indication. We propose a specific set of criteria to guide the decision-making around when to initiate human proof of principle without preclinical efficacy studies in animal models...
December 1, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29172645/a-homogeneous-cell-based-halide-sensitive-yellow-fluorescence-protein-assay-to-identify-modulators-of-the-cystic-fibrosis-transmembrane-conductance-regulator-ion-channel
#3
Emery Smith, Kenneth A Giuliano, Justin Shumate, Pierre Baillargeon, Brigid McEwan, Matthew D Cullen, John P Miller, Lawrence Drew, Louis Scampavia, Timothy P Spicer
Cystic fibrosis (CF), an inherited genetic disease, is caused by mutation of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) gene, which encodes an ion channel involved in hydration maintenance by anion homeostasis. Ninety percent of CF patients possess one or more copies of the F508del CFTR mutation. This mutation disrupts trafficking of the protein to the plasma membrane and diminishes function of mature CFTR. Identifying small molecule modulators of mutant CFTR activity or biosynthesis may yield new tools for discovering novel CF treatments...
November 27, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29148820/a-functional-kinase-short-interfering-ribonucleic-acid-screen-using-protease-activated-receptor-2-dependent-opening-of-transient-receptor-potential-vanilloid-4
#4
William G Darby, Megan S Grace, Kaylene J Simpson, Owen L Woodman, Peter McIntyre
Protease-activated receptor 2 (PAR2) is a proinflammatory G-protein coupled receptor (GPCR) that is activated by inflammatory proteases, and its activation initiates signaling pathways that modulate the nonselective cation channel transient receptor potential vanilloid-4 (TRPV4). PAR2-dependent opening of TRPV4 has been attributed to kinase activation, but the identity of the responsible enzymes is unknown. Deciphering the signaling pathways involved in the PAR2-dependent opening of TRPV4 may yield new targets for pain treatment...
November 17, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29112465/high-throughput-screening-identifies-1-4-5-substituted-1-2-3-triazole-analogs-as-potent-and-specific-antagonists-of-pregnane-x-receptor
#5
Wenwei Lin, Asli N Goktug, Jing Wu, Duane G Currier, Taosheng Chen
Human pregnane X receptor (hPXR) is a nuclear receptor that regulates the expression of phase I and phase II drug-metabolism enzymes, as well as that of drug transporters. hPXR is a "xenobiotics sensor" and can be activated by structurally diverse compounds. The activation of hPXR by its agonists increases the clearance of xenobiotics by increasing the expression of drug-metabolism enzymes and drug transporters, possibly leading to drug toxicity, drug resistance, and other adverse drug reactions. Therefore, hPXR antagonists might attenuate agonist-mediated activation of hPXR and reduce the risk of adverse drug reactions...
November 7, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29235897/old-compounds-new-uses-new-ways-many-ways
#6
Hermann Mucke
No abstract text is available yet for this article.
December 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29235896/drug-repurposing-patent-applications-april-june-2017
#7
Hermann A M Mucke
No abstract text is available yet for this article.
December 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29235895/drug-repurposing-patent-applications-july-september-2017
#8
Hermann A M Mucke
No abstract text is available yet for this article.
December 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29120675/utility-of-adenosine-monophosphate-detection-system-for-monitoring-the-activities-of-diverse-enzyme-reactions
#9
Subhanjan Mondal, Kevin Hsiao, Said A Goueli
Adenosine monophosphate (AMP) is a key cellular metabolite regulating energy homeostasis and signal transduction. AMP is also a product of various enzymatic reactions, many of which are dysregulated during disease conditions. Thus, monitoring the activities of these enzymes is a primary goal for developing modulators for these enzymes. In this study, we demonstrate the versatility of an enzyme-coupled assay that quantifies the amount of AMP produced by any enzymatic reaction regardless of its substrates. We successfully implemented it to enzyme reactions that use adenosine triphosphate (ATP) as a substrate (aminoacyl tRNA synthetase and DNA ligase) by an elaborate strategy of removing residual ATP and converting AMP produced into ATP; so it can be detected using luciferase/luciferin and generating light...
October 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29120674/overproduction-of-erythromycin-by-ultraviolet-mutagenesis-and-expression-of-erme-gene-in-saccharopolyspora-erythraea
#10
Nargis Fallahpour, Sanam Adnani, Hossein Rassi, Esmaeil Asli
Erythromycin is a macrolide antibiotic with broad-spectrum activity against gram-positive bacteria that stops protein synthesis by binding to 50s ribosomal subunit. Classical and recombinant strain improvement, such as application of ultraviolet (UV) mutagenesis and selection of overproduction mutant, is the most important and convenient method in enhancement of antibiotic production. In the present study, Saccharopolyspora erythraea was mutagenized using UV lights and selection by tylosin resistance mutant to improve yield of erythromycin...
October 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29120673/standard-curves-are-necessary-to-determine-pharmacological-properties-for-ligands-in-functional-assays-using-competition-binding-technologies
#11
Neil T Burford, John Watson, Andrew Alt
Homogeneous functional assays that utilize competition binding technology are widely used for determining pharmacological properties such as intrinsic activity and potency. One example is time-resolved fluorescence resonance energy transfer (TR-FRET) 3',5'-cyclic adenosine monophosphate (cAMP) assays, where labeled cAMP (tracer) and a labeled anti-cAMP antibody bind together to produce a TR-FRET signal when the two constituents are proximal to each other. This signal is disrupted when unlabeled and cellularly generated cAMP competes with the tracer cAMP for binding to the labeled antibody...
October 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29077483/risk-of-late-onset-alzheimer-s-disease-by-plasma-cholesterol-rational-in-silico-drug-investigation-of-pyrrole-based-hmg-coa-reductase-inhibitors
#12
Sajad Shahbazi, Jagdeep Kaur, Ananya Kuanar, Dattatreya Kar, Shikha Singh, Ranbir Chander Sobti
Alzheimer's disease (AD), a worldwide renowned progressive neurodegenerative disorder, is the most common cause of dementia. There are several studies on the important role of cholesterol metabolism in AD pathogenesis, which indicated that the high concentrations of serum cholesterol increase the risk of AD. Biosynthesis of the plasma cholesterol and other isoprenoids is catalyzed by 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCR) through the conversion of HMG-CoA to mevalonic acid in mevalonate pathway. Normally, the high level of plasma cholesterol is downregulated by HGMCR inhibition as the result of degradation of LDL, but in abnormal conditions, for example, high blood glucose, the HMGCR over activated resulting in uncontrolled blood cholesterol...
October 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29072843/literature-search-and-review
#13
Anton Simeonov, Doug Auld
No abstract text is available yet for this article.
October 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28891675/abstracts-the-society-of-biomolecular-imaging-and-informatics-4th-annual-meeting-poster-session-september-13-15-2017-san-diego-convention-center-san-diego-ca
#14
(no author information available yet)
No abstract text is available yet for this article.
September 11, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28891671/author-index-by-poster-number
#15
(no author information available yet)
No abstract text is available yet for this article.
September 11, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28837357/improving-comprehension-efficiency-of-high-content-screening-data-through-interactive-visualizations
#16
Wienand A Omta, Jacob de Nobel, Judith Klumperman, David A Egan, Marco R Spruit, Matthieu J S Brinkhuis
In this study, an experiment is conducted to measure the performance in speed and accuracy of interactive visualizations. A platform for interactive data visualizations was implemented using Django, D3, and Angular. Using this platform, a questionnaire was designed to measure a difference in performance between interactive and noninteractive data visualizations. In this questionnaire consisting of 12 questions, participants were given tasks in which they had to identify trends or patterns. Other tasks were directed at comparing and selecting algorithms with a certain outcome based on visualizations...
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28837356/phenotypic-assays-for-characterizing-compound-effects-on-induced-pluripotent-stem-cell-derived-cardiac-spheroids
#17
Oksana Sirenko, Michael K Hancock, Carole Crittenden, Matthew Hammer, Sean Keating, Coby B Carlson, Grischa Chandy
Development of more complex, biologically relevant, and predictive cell-based assays for compound screening is a major challenge in drug discovery. The focus of this study was to establish high-throughput compatible three-dimensional (3D) cardiotoxicity assays using human induced pluripotent stem cell-derived cardiomyocytes. Using both high-content imaging and fast kinetic fluorescence imaging, the impact of various compounds on the beating rates and patterns of cardiac spheroids was monitored by changes in intracellular Ca(2+) levels with calcium-sensitive dyes...
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28837355/society-of-biomolecular-imaging-and-informatics-special-issue
#18
Myles Fennell, Kaylene J Simpson
No abstract text is available yet for this article.
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28837354/society-of-biomolecular-imaging-and-informatics-4th-annual-meeting-september-13-15-2017
#19
(no author information available yet)
No abstract text is available yet for this article.
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28800248/how-phenotypic-screening-influenced-drug-discovery-lessons-from-five-years-of-practice
#20
Dorothea Haasen, Ulrich Schopfer, Christophe Antczak, Chantale Guy, Florian Fuchs, Paul Selzer
Since 2011, phenotypic screening has been a trend in the pharmaceutical industry as well as in academia. This renaissance was triggered by analyses that suggested that phenotypic screening is a superior strategy to discover first-in-class drugs. Despite these promises and considerable investments, pharmaceutical research organizations have encountered considerable challenges with the approach. Few success stories have emerged in the past 5 years and companies are questioning their investment in this area. In this contribution, we outline what we have learned about success factors and challenges of phenotypic screening...
August 2017: Assay and Drug Development Technologies
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