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Assay and Drug Development Technologies

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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
#1
(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
#2
(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/28742374/high-throughput-analysis-identifying-drugs-that-regulate-apolipoprotein-a-i-synthesis
#3
Michael J Haas, Luisa Onstead-Haas, William Kurban, Harshit Shah, Monica Plazarte, Ayham Chamseddin, Arshag D Mooradian
Apolipoprotein A-I (apo A-I) is the primary antiatherogenic protein in high-density lipoprotein (HDL). Despite the controversy as to the clinical effectiveness of raising HDL, the search is ongoing for safe and effective drugs that increase HDL and apo A-I levels. To identify novel compounds that can increase hepatic apo A-I production, two drug libraries were screened. The NIH clinical collection (NCC) and the NIH clinical collection 2 (NCC2) were purchased from Evotec (San Francisco, CA). The NCC library contains 446 compounds and the NCC2 library contains 281 compounds, all dissolved in dimethylsulfoxide at a concentration of 10 mM...
July 25, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28837357/improving-comprehension-efficiency-of-high-content-screening-data-through-interactive-visualizations
#4
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
#5
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
#6
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
#7
(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
#8
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
https://www.readbyqxmd.com/read/28800244/exploiting-analysis-of-heterogeneity-to-increase-the-information-content-extracted-from-fluorescence-micrographs-of-transgenic-zebrafish-embryos
#9
Tongying Shun, Albert H Gough, Subramaniam Sanker, Neil A Hukriede, Andreas Vogt
Zebrafish embryos are a near-ideal animal model for drug discovery because of their high genetic and physiological similarity to mammals, small size, high fecundity, and optical transparency. The latter properties make zebrafish at larval stages especially suited for high-content analysis and high throughput screening (HTS). However, inherent biological complexity and the inability to screen multiple specimens in a single well present a challenge for HTS because limiting replicates and high variability often prevent assays from reaching the stringent performance criteria demanded of large-scale screening assays...
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28771372/high-content-assay-multiplexing-for-vascular-toxicity-screening-in-induced-pluripotent-stem-cell-derived-endothelial-cells-and-human-umbilical-vein-endothelial-cells
#10
Yasuhiro Iwata, William D Klaren, Connie S Lebakken, Fabian A Grimm, Ivan Rusyn
Endothelial cells (ECs) play a major role in blood vessel formation and function. While there is longstanding evidence for the potential of chemical exposures to adversely affect EC function and vascular development, the hazard potential of chemicals with respect to vascular effects is not routinely evaluated in safety assessments. Induced pluripotent stem cell (iPSC)-derived ECs promise to provide a physiologically relevant, organotypic culture model that is amenable for high-throughput (HT) EC toxicant screening and may represent a viable alternative to traditional in vitro models, including human umbilical vein endothelial cells (HUVECs)...
August 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723272/literature-search-and-review
#11
Anton Simeonov, Mindy I Davis, Doug Auld
No abstract text is available yet for this article.
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723271/development-of-three-orthogonal-assays-suitable-for-the-identification-and-qualification-of-pikfyve-inhibitors
#12
Kylie Fogarty, Mohammed Kashem, Andras Bauer, Alexandra Bernardino, Debra Brennan, Brian Cook, Neil Farrow, Teresa Molinaro, Richard Nelson
FYVE-type zinc finger-containing phosphoinositide kinase (PIKfyve) catalyzes the formation of phosphatidylinositol 3,5-bisphosphate (PI(3,5)P2) from phosphatidylinositol 3-phosphate (PI(3)P). PIKfyve has been implicated in multiple cellular processes, and its role in the regulation of toll-like receptor (TLR) pathways and the production of proinflammatory cytokines has sparked interest in developing small-molecule PIKfyve inhibitors as potential therapeutics to treat autoimmune and inflammatory diseases. We developed three orthogonal assays to identify and qualify small-molecule inhibitors of PIKfyve: (1) a purified component microfluidic enzyme assay that measures the conversion of fluorescently labeled PI(3)P to PI(3,5)P2 by purified recombinant full-length human 6His-PIKfyve (rPIKfyve); (2) an intracellular protein stabilization assay using the kinase domain of PIKfyve expressed in HEK293 cells; and (3) a cell-based functional assay that measures the production of interleukin (IL)-12p70 in human peripheral blood mononuclear cells stimulated with TLR agonists lipopolysaccharide and R848...
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723270/in-the-july-2017-issue-of-assay%C3%A2
#13
Bruce Melancon
No abstract text is available yet for this article.
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723269/identification-of-antipneumococcal-molecules-effective-against-different-streptococcus-pneumoniae-serotypes-using-a-resazurin-based-high-throughput-screen
#14
Hyung Jun Kim, Namyoul Kim, David Shum, Srigouri Huddar, Chul Min Park, Soojin Jang
Streptococcus pneumoniae is a major human pathogen, causing around 1.6 million deaths worldwide each year. By optimizing a resazurin-based assay to detect S. pneumoniae growth in 384-well microplates, we developed a new high-throughput screening (HTS) system for the discovery of antipneumococcal molecules, which was unsuccessful using conventional absorbance measurements. Before applying our protocol to a large-scale screen, we validated the system through a pilot screen targeting about 7,800 bioactive molecules using three different S...
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28723268/assay-of-calcium-transients-and-synapses-in-rat-hippocampal-neurons-by-kinetic-image-cytometry-and-high-content-analysis-an-in-vitro-model-system-for-postchemotherapy-cognitive-impairment
#15
Patrick M McDonough, Natalie L Prigozhina, Ranor C B Basa, Jeffrey H Price
Postchemotherapy cognitive impairment (PCCI) is commonly exhibited by cancer patients treated with a variety of chemotherapeutic agents, including the endocrine disruptor tamoxifen (TAM). The etiology of PCCI is poorly understood. Our goal was to develop high-throughput assay methods to test the effects of chemicals on neuronal function applicable to PCCI. Rat hippocampal neurons (RHNs) were plated in 96- or 384-well dishes and exposed to test compounds (forskolin [FSK], 17β-estradiol [ES]), TAM or fulvestrant [FUL], aka ICI 182,780) for 6-14 days...
July 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28604056/literature-search-and-review
#16
Anton Simeonov, Doug Auld
No abstract text is available yet for this article.
June 12, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28631941/analytical-characterization-of-methyl-%C3%AE-cyclodextrin-for-pharmacological-activity-to-reduce-lysosomal-cholesterol-accumulation-in-niemann-pick-disease-type-c1-cells
#17
Rong Li, Jon Hao, Hideji Fujiwara, Miao Xu, Shu Yang, Sheng Dai, Yan Long, Manju Swaroop, Changhui Li, Mylinh Vu, Juan J Marugan, Daniel S Ory, Wei Zheng
Methyl-β-cyclodextrin (MβCD) reduces lysosomal cholesterol accumulation in Niemann-Pick disease type C1 (NPC1) patient fibroblasts. However, the pharmacological activity of MβCD reported by different laboratories varies. To determine the potential causes of this variation, we analyzed the mass spectrum characteristics, pharmacological activity of three preparations of MβCDs, and the protein expression profiles of NPC1 patient fibroblasts after treatment with different sources of MβCDs. Our data revealed varied mass spectrum profiles and pharmacological activities on the reduction of lysosomal cholesterol accumulation in NPC1 fibroblasts for these three preparations of MβCDs obtained from different batches and different sources...
May 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28631940/moving-forward-with-assay
#18
Bruce Melancon
No abstract text is available yet for this article.
May 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28631939/a-high-throughput-screening-assay-for-nkcc1-cotransporter-using-nonradioactive-rubidium-flux-technology
#19
Sikander Gill, Rajwant Gill, Yang Wen, Thilo Enderle, Doris Roth, Dong Liang
A high-throughput screening (HTS) assay was developed for cotransporter, NKCC1, which is a potential target for the treatment of diverse disorders. This nonradioactive rubidium flux assay coupled with ion channel reader series provides a working screen for this target expressed in human embryonic kidney (HEK) cell line. An eightfold window of detection was achieved with the optimized assay. This new functional assay offered a robust working model for NKCC1 in determining reliable and concordant rank orders of the test compounds supporting its sensitivity and specificity...
May 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28525289/high-throughput-phenotyping-of-human-induced-pluripotent-stem-cell-derived-cardiomyocytes-and-neurons-using-electric-field-stimulation-and-high-speed-fluorescence-imaging
#20
Neil J Daily, Zhong-Wei Du, Tetsuro Wakatsuki
Electrophysiology of excitable cells, including muscle cells and neurons, has been measured by making direct contact with a single cell using a micropipette electrode. To increase the assay throughput, optical devices such as microscopes and microplate readers have been used to analyze electrophysiology of multiple cells. We have established a high-throughput (HTP) analysis of action potentials (APs) in highly enriched motor neurons and cardiomyocytes (CMs) that are differentiated from human induced pluripotent stem cells (iPSCs)...
May 2017: Assay and Drug Development Technologies
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