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High throughput screen

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https://www.readbyqxmd.com/read/28231433/discovery-of-a-potent-and-selective-sphingosine-kinase-1-inhibitor-through-the-molecular-combination-of-chemotype-distinct-screening-hits
#1
Mark E Schnute, Matthew D McReynolds, Jeffrey Carroll, Jill E Chrencik, Maureen K Highkin, Kaliapan Iyanar, Gina Jerome, John W Rains, Matthew Saabye, Jeffrey A Scholten, Matthew Yates, Marek M Nagiec
Sphingosine kinase (SphK) is the major source of the lipid mediator and GPCR agonist sphingosine-1-phosphate (S1P). S1P promotes cell growth, survival and migration and is a key regulator of lymphocyte trafficking. Inhibition of S1P signaling has been proposed as a strategy for treatment of inflammatory diseases and cancer. Two different formats of an enzyme based high-throughput screen yielded two attractive chemotypes capable of inhibiting S1P formation in cells. The molecular combination of these screening hits led to compound 22a (PF-543) with two orders of magnitude improved potency...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231319/development-of-a-keratinase-activity-assay-using-recombinant-chicken-feather-keratin-substrates
#2
Hyeon-Su Jin, Seon Yeong Park, Kyungmin Kim, Yong-Jik Lee, Gae-Won Nam, Nam Joo Kang, Dong-Woo Lee
Poultry feathers consist mainly of the protein keratin, which is rich in β-pleated sheets and consequently resistant to proteolysis. Although many keratinases have been identified, the reasons for their substrate specificity towards β-keratin remain unclear due to difficulties in preparing a soluble feather keratin substrate for use in activity assays. In the present study, we overexpressed Gallus gallus chromosomes 2 and 27 β-keratin-encoding genes in Escherichia coli, purified denatured recombinant proteins by Ni2+ affinity chromatography, and refolded by stepwise dialysis to yield soluble keratins...
2017: PloS One
https://www.readbyqxmd.com/read/28231034/upscaling-of-hips-cell-derived-neurons-for-high-throughput-screening
#3
Stefanie Traub, Heiko Stahl, Holger Rosenbrock, Eric Simon, Ralf Heilker
The advent of human-induced pluripotent stem (hiPS) cell-derived neurons promised to provide better model cells for drug discovery in the context of the central nervous system. This work demonstrates both the upscaling of cellular expansion and the acceleration of neuronal differentiation to accommodate the immense material needs of a high-throughput screening (HTS) approach. Using GRowth factor-driven expansion and INhibition of NotCH (GRINCH) during maturation, the derived cells are here referred to as GRINCH neurons...
March 2017: SLAS Discov
https://www.readbyqxmd.com/read/28231025/rabit-ii-implementation-of-a-high-throughput-micronucleus-biodosimetry-assay-on-commercial-biotech-robotic-systems
#4
Mikhail Repin, Sergey Pampou, Charles Karan, David J Brenner, Guy Garty
We demonstrate the use of high-throughput biodosimetry platforms based on commercial high-throughput/high-content screening robotic systems. The cytokinesis-block micronucleus (CBMN) assay, using only 20 μl whole blood from a fingerstick, was implemented on a PerkinElmer cell::explorer and General Electric IN Cell Analyzer 2000. On average 500 binucleated cells per sample were detected by our FluorQuantMN software. A calibration curve was generated in the radiation dose range up to 5.0 Gy using the data from 8 donors and 48,083 binucleated cells in total...
February 23, 2017: Radiation Research
https://www.readbyqxmd.com/read/28230985/discovery-of-competitive-and-non-competitive-ligands-of-the-organic-cation-transporter-1-oct1-slc22a1
#5
Eugene C Chen, Natalia Khuri, Xiaomin Liang, Adrian Stecula, Huan-Chieh Chien, Sook Wah Yee, Yong Huang, Andrej Sali, Kathleen M Giacomini
Organic cation transporter 1 (OCT1) plays a critical role in the hepatocellular uptake of structurally diverse endogenous compounds and xenobiotics. Here, we identified competitive and noncompetitive OCT1 interacting ligands in a library of 1,780 prescription drugs by combining in silico and in vitro methods. Ligands were predicted by docking against a comparative model based a eukaryotic homolog. In parallel, high-throughput screening (HTS) was conducted using the fluorescent probe substrate ASP+ in cells overexpressing human OCT1...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28229947/high-throughput-screening-and-scale-up-of-cocrystals-using-resonant-acoustic-mixing
#6
Karthik Nagapudi, Evelyn Yanez Umanzor, Colin Masui
This paper explores the effectiveness of resonant acoustic mixing RAM for screening and scale up of cocrystals 16 cocrystal systems were selected as test cases based on previous literature precedent A 96 well plate set up in conjunction with zirconia beads was used for cocrystal screening using RAM A success rate of 80% was obtained in the screen for plates containing solvent or solvent plus Zirconia beads A proof of concept production of hydrated and anhydrous cocrystals of 1:1 Theophylline Citric acid system at a 400mg scale was demonstrated using solvent and bead assisted RAM Finally the parameters affecting the scale up of 2:1 Theophylline Oxalic acid cocrystals was explored in a systematic fashion using a Design of Experiments DOE approach The RAM parameters of acceleration and mixing time were optimized using the DOE approach A quantitative XRPD method was developed to determine the extent of conversion to the cocrystal when using RAM Mixing time of 2hours and an acceleration of 60 G were determined to be optimal The optimized parameters were used to demonstrate scale up of 2:1 Theophylline Oxalic acid cocrystals at an 80 gram scale with a net yield of 94% RAM is thus established as an environmentally friendly mechanochemical technique for both high throughput screening and scaled up production of cocrystals...
February 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28228596/antimicrobials-from-human-skin-commensal-bacteria-protect-against-staphylococcus-aureus-and-are-deficient-in-atopic-dermatitis
#7
Teruaki Nakatsuji, Tiffany H Chen, Saisindhu Narala, Kimberly A Chun, Aimee M Two, Tong Yun, Faiza Shafiq, Paul F Kotol, Amina Bouslimani, Alexey V Melnik, Haythem Latif, Ji-Nu Kim, Alexandre Lockhart, Keli Artis, Gloria David, Patricia Taylor, Joanne Streib, Pieter C Dorrestein, Alex Grier, Steven R Gill, Karsten Zengler, Tissa R Hata, Donald Y M Leung, Richard L Gallo
The microbiome can promote or disrupt human health by influencing both adaptive and innate immune functions. We tested whether bacteria that normally reside on human skin participate in host defense by killing Staphylococcus aureus, a pathogen commonly found in patients with atopic dermatitis (AD) and an important factor that exacerbates this disease. High-throughput screening for antimicrobial activity against S. aureus was performed on isolates of coagulase-negative Staphylococcus (CoNS) collected from the skin of healthy and AD subjects...
February 22, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/28228269/diverse-central-projection-patterns-of-retinal-ganglion-cells
#8
Emily M Martersteck, Karla E Hirokawa, Mariah Evarts, Amy Bernard, Xin Duan, Yang Li, Lydia Ng, Seung W Oh, Benjamin Ouellette, Joshua J Royall, Michelle Stoecklin, Quanxin Wang, Hongkui Zeng, Joshua R Sanes, Julie A Harris
Understanding how >30 types of retinal ganglion cells (RGCs) in the mouse retina each contribute to visual processing in the brain will require more tools that label and manipulate specific RGCs. We screened and analyzed retinal expression of Cre recombinase using 88 transgenic driver lines. In many lines, Cre was expressed in multiple RGC types and retinal cell classes, but several exhibited more selective expression. We comprehensively mapped central projections from RGCs labeled in 26 Cre lines using viral tracers, high-throughput imaging, and a data processing pipeline...
February 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/28227433/microprinted-tumor-spheroids-enable-anti-cancer-drug-screening
#9
Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Stephanie L Ham, Hossein Tavana
Spheroids present a biologically relevant model of avascular tumors and a unique tool for discovery of anti-cancer drugs. Despite being used in research laboratories for several decades, spheroids are not routinely used for drug discovery primarily due to the difficulty of mass-producing uniformly-sized spheroids and intense labor involved in handling, drug treatment, and analyzing them. We overcome this barrier using a novel technology to robotically microprint spheroids in standard 384-well plates. An aqueous drop containing cancer cells is dispensed into a bath of a second, immiscible aqueous phase...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28225116/high-throughput-drawing-and-testing-of-metallic-glass-nanostructures
#10
Molla Hasan, Golden Kumar
Thermoplastic embossing of metallic glasses promises direct imprinting of metal nanostructures using templates. However, embossing high-aspect-ratio nanostructures faces unworkable flow resistance due to friction and non-wetting conditions at the template interface. Herein, we show that these inherent challenges of embossing can be reversed by thermoplastic drawing using templates. The flow resistance not only remains independent of wetting but also decreases with increasing feature aspect-ratio. Arrays of assembled nanotips, nanowires, and nanotubes with aspect-ratios exceeding 1000 can be produced through controlled elongation and fracture of metallic glass structures...
February 22, 2017: Nanoscale
https://www.readbyqxmd.com/read/28224912/high-throughput-screening-and-quantitation-of-guanidino-and-ureido-compounds-using-liquid-chromatography-drift-tube-ion-mobility-spectrometry-mass-spectrometry
#11
Ruo-Jing Fan, Fang Zhang, Xiu-Ping Chen, Wan-Shu Qi, Qing Guan, Tuan-Qi Sun, Yin-Long Guo
The present work focused on the high-throughput screening and quantitation of guanidino compounds (GCs) and ureido compounds (UCs) in human thyroid tissues. The strategy employed benzylic rearrangement stable isotope labeling (BRSIL) for the sample preparation and then detection using liquid chromatography-drift tube ion mobility spectrometry-quadrupole time of flight mass spectrometry (LC-DTIMS-QTOF MS). A short reversed-phase LC realized an on-line desalting and a measurement cycle of 5.0 min. DTIMS separation enhanced the better specificity and selectivity for the benzil labeled GCs and UCs...
April 8, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28224461/zinc-the-other-suspected-environmental-factor-in-kashin-beck-disease-in-addition-to-selenium
#12
REVIEW
Xi Wang, Yujie Ning, Lei Yang, Fangfang Yu, Xiong Guo
Kashin-Beck disease (KBD) is an endemic chronic osteochondral disease characterized by high prevalence, disability, and morbidity and is distributed from the northeast to the southwest in China, in some regions of Eastern Siberia in Russia, and in North Korea. Although the selenium deficiency etiological hypothesis for KBD has been proposed by scientists for decades, the idea that selenium deficiency is one of the most important environmental factors but not the primary and sole pathogenic factor for KBD has been widely accepted...
February 21, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/28223509/high-throughput-screening-of-rare-metabolically-active-tumor-cells-in-pleural-effusion-and-peripheral-blood-of-lung-cancer-patients
#13
Yin Tang, Zhuo Wang, Ziming Li, Jungwoo Kim, Yuliang Deng, Yan Li, James R Heath, Wei Wei, Shun Lu, Qihui Shi
Malignant pleural effusion (MPE), the presence of malignant cells in pleural fluid, is often the first sign of many cancers and occurs in patients with metastatic malignancies. Accurate detection of tumor cells in pleural fluid is crucial because the presence of MPE denotes an advanced stage of disease and directs a switch in clinical managements. Cytology, as a traditional diagnostic tool, has limited sensitivity especially when tumor cells are not abundant, and may be confounded by reactive mesothelial cells in the pleural fluid...
February 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28223377/exopolysaccharide-repressing-small-molecules-with-antibiofilm-and-antivirulence-activity-against-pseudomonas-aeruginosa
#14
Erik van Tilburg Bernardes, Laetitia Charron-Mazenod, David J Reading, Shauna L Reckseidler-Zenteno, Shawn Lewenza
Biofilm formation is a universal virulence strategy in which bacteria grow in dense microbial communities enmeshed within a polymeric extracellular matrix that protects them from antibiotic exposure and the immune system. Pseudomonas aeruginosa is an archetypal biofilm-forming organism that utilizes a biofilm growth strategy to cause chronic lung infections in Cystic Fibrosis (CF) patients. The extracellular matrix of P. aeruginosa biofilms is comprised mainly of exopolysaccharides (EPS) and DNA. Both mucoid and non-mucoid isolates of P...
February 21, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28223349/identification-of-antibody-targets-for-tuberculosis-serology-using-high-density-nucleic-acid-programmable-protein-arrays
#15
Lusheng Song, Garrick Wallstrom, Xiaobo Yu, Marika Hopper, Jennifer Van Duine, Jason Steel, Jin Park, Peter Wiktor, Peter Khan, Al Brunner, Douglas Wilson, Elizabeth R Jenny-Avital, Ji Qiu, Joshua LaBaer, D Mitchell Magee, Jacqueline M Achkar
Better and more diverse biomarkers for the development of simple point-of-care tests for active tuberculosis (TB), a clinically heterogeneous disease, are urgently needed. We generated a proteomic Mycobacterium tuberculosis (Mtb) High-Density Nucleic Acid Programmable Protein Array (HD-NAPPA) that used a novel multiplexed strategy for expedited high-throughput screening for antibody responses to the Mtb proteome. We screened sera from HIV uninfected and co-infected TB patients and controls (n = 120) from the US and South Africa (SA) using the multiplex HD-NAPPA for discovery, followed by deconvolution and validation through single protein HD-NAPPA with biologically independent samples (n=124)...
February 21, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28223164/exploring-sensitivity-throughput-of-a-parallel-flow-spri-biosensor-for-characterization-of-antibody-antigen-interaction
#16
Vishal Kamat, Ashique Rafique
Rapid growth in the field of biotherapeutics has led to an increased demand for high-throughput, label-free biosensors exhibiting high sensitivity. To support the current needs, Sierra Sensors introduced a surface plasmon resonance imaging (SPRi) based biosensor, Molecular Affinity Screening System (MASS-1). We assessed the potential utility of MASS-1 to support Regeneron's therapeutic antibody discovery. A large panel of antibody-antigen interactions was characterized using MASS-1 and the kinetic data were compared with the Biacore 4000 biosensor...
February 18, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28223069/evaluation-of-antibacterial-potential-and-toxicity-of-plant-volatile-compounds-using-new-broth-microdilution-volatilization-method-and-modified-mtt-assay
#17
Marketa Houdkova, Johana Rondevaldova, Ivo Doskocil, Ladislav Kokoska
With aim to develop effective proof-of-concept approach which can be used in a development of new preparations for the inhalation therapy, we designed a new screening method for simple and rapid simultaneous determination of antibacterial potential of plant volatiles in the liquid and the vapour phase at different concentrations. In addition, EVA (ethylene vinyl acetate) capmat™ as vapour barrier cover was used as reliable modification of thiazolyl blue tetrazolium bromide (MTT) assay for cytotoxicity testing of volatiles on microtiter plates...
February 18, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28222744/herpes-simplex-virus-1-infection-dampens-the-immediate-early-antiviral-innate-immunity-signaling-from-peroxisomes-by-tegument-protein-vp16
#18
Chunfu Zheng, Chenhe Su
BACKGROUND: Herpes simplex virus 1 (HSV-1) is an archetypal member of the alphaherpesvirus subfamily with a large genome encoding over 80 proteins, many of which play a critical role in virus-host interactions and immune modulation. Upon viral infections, the host cells activate innate immune responses to restrict their replications. Peroxisomes, which have long been defined to regulate metabolic activities, are reported to be important signaling platforms for antiviral innate immunity...
February 21, 2017: Virology Journal
https://www.readbyqxmd.com/read/28222617/presynaptic-calmodulin-targets-lessons-from-structural-proteomics
#19
Noa Lipstein, Melanie Göth, Christine Piotrowski, Kevin Pagel, Andrea Sinz, Olaf Jahn
Calmodulin (CaM) is a highly conserved Ca(2+)-binding protein that is exceptionally abundant in the brain. In the presynaptic compartment of neurons, CaM transduces changes in Ca(2+) concentration into the regulation of synaptic transmission dynamics. Areas covered: We review selected literature including published CaM interactor screens and outline established and candidate presynaptic CaM targets. We present a workflow of biochemical and structural proteomic methods that were used to identify and characterize the interactions between CaM and Munc13 proteins...
March 2017: Expert Review of Proteomics
https://www.readbyqxmd.com/read/28222202/tsc1-and-tsc2-gene-mutations-and-their-implications-for-treatment-in-tuberous-sclerosis-complex-a-review
#20
Clévia Rosset, Cristina Brinckmann Oliveira Netto, Patricia Ashton-Prolla
Tuberous sclerosis complex is an autosomal dominant disorder characterized by skin manifestations and formation of multiple tumors in different organs, mainly in the central nervous system. Tuberous sclerosis is caused by the mutation of one of two tumor suppressor genes, TSC1 or TSC2. Currently, the development of novel techniques and great advances in high-throughput genetic analysis made mutation screening of the TSC1 and TSC2 genes more widely available. Extensive studies of the TSC1 and TSC2 genes in patients with TSC worldwide have revealed a wide spectrum of mutations...
February 20, 2017: Genetics and Molecular Biology
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