keyword
MENU ▼
Read by QxMD icon Read
search

High throughput screen

keyword
https://www.readbyqxmd.com/read/28324707/chemical-structure-based-predictive-model-for-the-oxidation-of-trace-organic-contaminants-by-sulfate-radical
#1
Tiantian Ye, Zongsu Wei, Richard Spinney, Chong-Jian Tang, Shuang Luo, Ruiyang Xiao, Dionysios D Dionysiou
Second-order rate constants [Formula: see text] for the reaction of sulfate radical anion (SO4(•-)) with trace organic contaminants (TrOCs) are of scientific and practical importance for assessing their environmental fate and removal efficiency in water treatment systems. Here, we developed a chemical structure-based model for predicting [Formula: see text] using 32 molecular fragment descriptors, as this type of model provides a quick estimate at low computational cost. The model was constructed using the multiple linear regression (MLR) and artificial neural network (ANN) methods...
March 6, 2017: Water Research
https://www.readbyqxmd.com/read/28324660/single-and-combination-drug-screening-with-aqueous-biphasic-tumor-spheroids
#2
Pradip Shahi Thakuri, Hossein Tavana
Spheroids of cancer cells represent a physiologic model of solid tumors for cancer drug screening. Despite this known benefit, difficulties with generating large quantities of uniformly sized spheroids in standard plates, individually addressing spheroids with drug compounds, and quantitatively analyzing responses of cancer cells have hindered the use of spheroids in high-throughput screening applications. Recently, we addressed this challenge by using an aqueous two-phase system technology to generate a spheroid within an aqueous drop immersed in a second, immiscible aqueous phase...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28324614/fluorescence-based-high-throughput-and-targeted-image-acquisition-and-analysis-for-phenotypic-screening
#3
Manuel Gunkel, Jan Philipp Eberle, Holger Erfle
Applying the right acquisition method in a fluorescence imaging-based screening context is of great importance to obtain an appropriate readout and to select the right scale of the screen. In order to save imaging time and data, we have developed routines for multiscale targeted imaging, providing both a broad overview of a sample and additional in-depth information for targets of interest identified within the screen. These objects can be identified and acquired on-the-fly by an interconnection of image acquisition and image analysis...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28324501/assessing-telomerase-activities-in-mammalian-cells-using-the-quantitative-pcr-based-telomeric-repeat-amplification-protocol-qtrap
#4
Shuai Jiang, Mengfan Tang, Huawei Xin, Junjiu Huang
Telomerase expression and activity appear elevated in >80% of human cancers. The activity of the telomerase may serve as a diagnostic marker for malignancy, and an indicator of the proliferative potential of somatic and stem cells. The telomeric repeat amplification protocol (TRAP) is a sensitive and accurate PCR-based assay for telomerase detection and measurement. Here, we describe a quantitative PCR-based TRAP assay (qTRAP) that is more convenient and amenable to high-throughput applications compared to traditional gel-based TRAP assays...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28324498/telomere-g-overhang-length-measurement-method-2-g-tail-telomere-hpa
#5
Hidetoshi Tahara
Both telomere length and telomere G-tail length are altered in human diseases such as cancer and age-related diseases. While most methods for measurement of G-tail and telomere length require electrophoresis, centrifugation, radioisotope labeling and autoradiography, G-tail telomere HPA provides a convenient and useful tool for the examination of G-tail length with a high-throughput platform using genomic DNA or cell lysate. G-tail telomere HPA may be applicable for clinical diagnostics as well as drug target screening...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28323890/establishment-of-transient-gene-expression-systems-in-protoplasts-from-liriodendron-hybrid-mesophyll-cells
#6
Ailing Huo, Zhenyu Chen, Pengkai Wang, Liming Yang, Guangping Wang, Dandan Wang, Suchan Liao, Tielong Cheng, Jinhui Chen, Jisen Shi
Liriodendron is a genus of the magnolia family comprised of two flowering tree species that produce hardwoods of great ecological and economic value. However, only a limited amount of genetic research has been performed on the Liriodendron genus partly because transient or stable transgenic trees have been difficult to produce. In general, transient expression systems are indispensable for rapid, high-throughput screening and systematic characterization of gene functions at a low cost; therefore, development of such a system for Liriodendron would provide a necessary step forward for research on Magnoliaceae and other woody trees...
2017: PloS One
https://www.readbyqxmd.com/read/28319085/synergistic-drug-combinations-for-cancer-identified-in-a-crispr-screen-for-pairwise-genetic-interactions
#7
Kyuho Han, Edwin E Jeng, Gaelen T Hess, David W Morgens, Amy Li, Michael C Bassik
Identification of effective combination therapies is critical to address the emergence of drug-resistant cancers, but direct screening of all possible drug combinations is infeasible. Here we introduce a CRISPR-based double knockout (CDKO) system that improves the efficiency of combinatorial genetic screening using an effective strategy for cloning and sequencing paired single guide RNA (sgRNA) libraries and a robust statistical scoring method for calculating genetic interactions (GIs) from CRISPR-deleted gene pairs...
March 20, 2017: Nature Biotechnology
https://www.readbyqxmd.com/read/28318945/identification-and-structure-activity-relationships-of-quinoline-tertiary-alcohol-modulators-of-ror%C3%AE-t
#8
David A Kummer, Maxwell D Cummings, Marta Abad, Joseph Barbay, Glenda Castro, Ronald Wolin, Kevin D Kreutter, Umar Maharoof, Cynthia Milligan, Rachel Nishimura, Joan Pierce, Celine Schalk-Hihi, John Spurlino, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Craig Woods, Xiaohua Xue, James P Edwards, Anne M Fourie, Kristi Leonard
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.
February 21, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28318223/high-throughput-dual-screening-method-for-ras-activities-and-inhibitors
#9
Kari Kopra, Arjan J van Adrichem, Outi M H Salo-Ahen, Juha Peltonen, Krister Wennerberg, Harri J Härmä
Ras GTPases act as "molecular switches", alternating between inactive GDP-bound and active GTP-bound conformation. Ras-oncogenes were discovered over three decades ago, but there are still no effective therapies for Ras-driven cancers. Drug discovery strategies have so far been unsuccessful, due to a lack of suitable screening methodologies and well-defined binding pockets on the Ras proteins. Here, we addressed the former by introducing a homogeneous quenching resonance energy transfer (QRET) technique based screening strategy for Ras interfacial and competitive inhibitors...
March 20, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28317854/sets-of-serum-exosomal-micrornas-as-candidate-diagnostic-biomarkers-for-kawasaki-disease
#10
Hong-Ling Jia, Chao-Wu Liu, Li Zhang, Wei-Jun Xu, Xue-Juan Gao, Jun Bai, Yu-Fen Xu, Ming-Guo Xu, Gong Zhang
Although Kawasaki disease is the main cause of acquired heart disease in children, no diagnostic biomarkers are available. We aimed to identify candidate biomarkers for diagnosing Kawasaki disease using serum exosomal microRNAs (miRNAs). Using frozen serum samples from a biobank, high-throughput microarray technologies, two-stage real-time quantitative PCR, and a self-referencing strategy for data normalization, we narrowed down the list of biomarker candidates to a set of 4 miRNAs. We further validated the diagnostic capabilities of the identified miRNAs (namely, CT(miR-1246)-CT(miR-4436b-5p) and CT(miR-197-3p)-CT(miR-671-5p)) in 79 samples from two hospitals...
March 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28317242/chemical-screening-identifies-rock-as-a-target-for-recovering-mitochondrial-function-in-hutchinson-gilford-progeria-syndrome
#11
Hyun Tae Kang, Joon Tae Park, Kobong Choi, Hyo Jei Claudia Choi, Chul Won Jung, Gyu Ree Kim, Young-Sam Lee, Sang Chul Park
Hutchinson-Gilford progeria syndrome (HGPS) constitutes a genetic disease wherein an aging phenotype manifests in childhood. Recent studies indicate that reactive oxygen species (ROS) play important roles in HGPS phenotype progression. Thus, pharmacological reduction in ROS levels has been proposed as a potentially effective treatment for patient with this disorder. In this study, we performed high-throughput screening to find compounds that could reduce ROS levels in HGPS fibroblasts and identified rho-associated protein kinase (ROCK) inhibitor (Y-27632) as an effective agent...
March 19, 2017: Aging Cell
https://www.readbyqxmd.com/read/28315670/sulfatase-activity-assay-using-an-activity-based-probe-by-generation-of-n-methyl-isoindole-under-reducing-conditions
#12
Hey Young Yoon, Jong-In Hong
Sulfatases catalyze the hydrolysis of sulfate esters that are present in a range of biomolecules. This is an important step in several biological processes such as cellular degradation, hormone regulation, and cell signaling. We have developed a new activity-based sulfatase probe (probe 1) that generates a fluorescent N-methylisoindole upon hydrolysis by sulfatase. Because of the autoxidation of N-methylisoindole, the sulfatase activity was also tested under reducing conditions, containing either glutathione (GSH) or tris(2-carboxyethyl)phosphine (TCEP), exhibiting little change in kinetic parameters compared to non-reducing conditions...
March 15, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28315326/identification-of-parp14-inhibitors-using-novel-methods-for-detecting-auto-ribosylation
#13
Mariko Yoneyama-Hirozane, Shin-Ichi Matsumoto, Yukio Toyoda, Singh Saikatendu Kumar, Yumi Zama, Kazuko Yonemori, Motomi Oonishi, Tsuyoshi Ishii, Tomohiro Kawamoto
Poly(ADP-ribose) polymerases (PARPs) use nicotinamide adenine dinucleotide (NAD(+)) as a co-substrate to transfer ADP-ribose when it releases nicotinamide as the metabolized product. Enzymes of the PARP family play key roles in detecting and repairing DNA, modifying chromatin, regulating transcription, controlling energy metabolism, and inducing cell death. PARP14, the original member of the PARP family, has been reported to be associated with the development of inflammatory diseases and various cancer types, making it a potential therapeutic target...
March 14, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28315072/direct-myosin-activation-by-omecamtiv-mecarbil-for-heart-failure-with-reduced-ejection-fraction
#14
Mitchell A Psotka, John R Teerlink
Myosin is the indispensable molecular motor that utilizes chemical energy to produce force for contraction within the cardiac myocyte. Myosin activity is gated by intracellular calcium levels which are regulated by multiple upstream signaling cascades that can be altered for clinical utility using inotropic medications. In contrast to clinically available cardiac inotropes, omecamtiv mecarbil is a novel direct myosin activator developed to augment left ventricular systolic function without the undesirable secondary effects of altered calcium homeostasis...
March 18, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28314411/small-molecule-inhibition-of-interleukin-1-receptor-associated-kinase-4-irak4
#15
N E Genung, K M Guckian
In recent years, interleukin-1 receptor-associated kinase 4, IRAK4, has become an attractive target for many medicinal chemistry programmes. Target inhibition is of potential therapeutic value in areas including autoimmune disorders, cancer, inflammatory diseases, and possibly neurodegenerative diseases. Results from high-throughput screening efforts have led, in conjunction with structure-based drug design, to the identification of highly potent and selective small molecule IRAK4 inhibitors from many diverse chemical series...
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28314120/a-systematic-approach-to-identify-biased-agonists-of-the-apelin-receptor-through-high-throughput-screening
#16
Danielle McAnally, Khandaker Siddiquee, Haleli Sharir, Feng Qi, Sharangdhar Phatak, Jian-Liang Li, Eric Berg, Jordan Fishman, Layton Smith
Biased agonists are defined by their ability to selectively activate distinct signaling pathways of a receptor, and they hold enormous promise for the development of novel drugs that specifically elicit only the desired therapeutic response and avoid potential adverse effects. Unfortunately, most high-throughput screening (HTS) assays are designed to detect signaling of G protein-coupled receptors (GPCRs) downstream of either G protein or β-arrestin-mediated signaling but not both. A comprehensive drug discovery program seeking biased agonists must employ assays that report on the activity of each compound at multiple discrete pathways, particularly for HTS campaigns...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28314118/in-vitro-assay-development-and-hts-of-small-molecule-human-abad-17%C3%AE-hsd10-inhibitors-as-therapeutics-in-alzheimer-s-disease
#17
Laura Aitken, Gemma Baillie, Andrew Pannifer, Angus Morrison, Philip S Jones, Terry K Smith, Stuart P McElroy, Frank J Gunn-Moore
A major hallmark of Alzheimer's disease (AD) is the formation of neurotoxic aggregates composed of the amyloid-β peptide (Aβ). Aβ has been recognized to interact with numerous proteins, resulting in pathological changes to the metabolism of patients with AD. One such mitochondrial metabolic enzyme is amyloid-binding alcohol dehydrogenase (ABAD), where altered enzyme function caused by the Aβ-ABAD interaction is known to cause mitochondrial distress and cytotoxic effects, providing a feasible therapeutic target for AD drug development...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28304162/rational-design-synthesis-and-biological-evaluation-of-heterocyclic-quinolones-targeting-the-respiratory-chain-of-mycobacterium-tuberculosis
#18
Weiqian David Hong, Peter D Gibbons, Suet C Leung, Richard Amewu, Paul A Stocks, Andrew Valentine Stachulski, Pedro C Horta, Maria Lurdes Santos Cristiano, Alison E Shone, Darren Moss, Alison Ardrey, Raman Sharma, Ashley J Warman, Paul T P Bedingfield, Nicholas E Fisher, Ghaith Aljayyoussi, Sally Mead, Maxine Caws, Neil G Berry, Stephen A Ward, Giancarlo A Biagini, Paul M O'Neill, Gemma Louise Nixon
A High-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). 11,000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11,000 compounds) and in-house screening of a limited number of quinolones (50 compounds) identified ~100 hits and four distinct chemotypes, the most promising of which contained the quinolone core...
March 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28303936/all-passive-pixel-super-resolution-of-time-stretch-imaging
#19
Antony C S Chan, Ho-Cheung Ng, Sharat C V Bogaraju, Hayden K H So, Edmund Y Lam, Kevin K Tsia
Based on image encoding in a serial-temporal format, optical time-stretch imaging entails a stringent requirement of state-of-the-art fast data acquisition unit in order to preserve high image resolution at an ultrahigh frame rate - hampering the widespread utilities of such technology. Here, we propose a pixel super-resolution (pixel-SR) technique tailored for time-stretch imaging that preserves pixel resolution at a relaxed sampling rate. It harnesses the subpixel shifts between image frames inherently introduced by asynchronous digital sampling of the continuous time-stretch imaging process...
March 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28303392/lettuce-flavonoids-screening-and-phenotyping-by-chlorophyll-fluorescence-excitation-ratio
#20
Marek Zivcak, Klaudia Brückova, Oksana Sytar, Marian Brestic, Katarina Olsovska, Suleyman I Allakhverdiev
Environmentally induced variation and the genotypic differences in flavonoid and phenolic content in lettuce can be reliably detected using the appropriate parameters derived from the records of rapid non-invasive fluorescence technique. The chlorophyll fluorescence excitation ratio method was designed as a rapid and non-invasive tool to estimate the content of UV-absorbing phenolic compounds in plants. Using this technique, we have assessed the dynamics of accumulation of flavonoids related to developmental changes and environmental effects...
March 16, 2017: Planta
keyword
keyword
38522
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"