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Journal articles on the topic 'High-throughput compound screening'

Author: Grafiati

Published: 4 June 2021

Last updated: 6 February 2022

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1

Gosnell, Paul A., Amy D. Hilton, Lynette M. Anderson, Lyman Wilkins, and William P. Janzen. "Compound Library Management in High Throughput Screening." Journal of Biomolecular Screening 2, no. 2 (1997): 99–102. http://dx.doi.org/10.1177/108705719700200208.

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Compound library management is inherent to the success of a high throughput screen. The library management system developed at Sphinx Pharmaceuticals accomplishes this through a series of Paradox and Orade database applications. This suite of applications allows compounds to be grouped as libraries, inventoried, and scheduled for testing in a screen. Compound libraries can be defied using any combination of source, structure, and target, and may be divided into sublibraries, allowing a flexible mix of compounds to be scheduled across several targets. Test requests can then be made for an entir

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2

Entzeroth, Michael, Béatrice Chapelain, Jacques Guilbert, and Valérie Hamon. "High throughput drug profiling." Journal of Automated Methods and Management in Chemistry 22, no. 6 (2000): 171–73. http://dx.doi.org/10.1155/s1463924600000304.

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High throughput screening has significantly contributed to advances in drug discovery. The great increase in the number of samples screened has been accompanied by increases in costs and in the data required for the investigated compounds. High throughput profiling addresses the issues of compound selectivity and specificity. It combines conventional screening with data mining technologies to give a full set of data, enabling development candidates to be more fully compared.

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3

Astle, Thomas W. "MicroTape-A 384-Well Ultra High Throughput Screening System." JALA: Journal of the Association for Laboratory Automation 4, no. 2 (1999): 31–34. http://dx.doi.org/10.1177/221106829900400207.

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The use of a sprocket driven carrier tape provides a unique solution for Ultra High Throughput Screening. 10-microliter wells in the 384 well pattern are embossed in a polypropylene or polycarbonate carrier tape. For compound handling, 100,000 compounds in 5 microliter aliquots may be stored, sealed and frozen in a roll 16 inches in diameter and 4 inches wide. The sprocket drive provides recall to any given compound. At time of use, the peelable seal is removed for access to the compound aliquots. Two levels of assay automation are provided. In Phase I the compound MicroTape is used to support

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4

Hansen, Clinton H. "High-Throughput Compound Screening using DNA Nanoswitches." Biophysical Journal 110, no. 3 (2016): 653a. http://dx.doi.org/10.1016/j.bpj.2015.11.3496.

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5

YASGAR, A. "Compound Management for Quantitative High-Throughput Screening." Journal of the Association for Laboratory Automation 13, no. 2 (2008): 79–89. http://dx.doi.org/10.1016/j.jala.2007.12.004.

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Patel, Dhara A., Anand C. Patel, William C. Nolan, et al. "High-Throughput Screening Normalized to Biological Response." Journal of Biomolecular Screening 19, no. 1 (2013): 119–30. http://dx.doi.org/10.1177/1087057113496848.

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The process of conducting cell-based phenotypic screens can result in data sets from small libraries or portions of large libraries, making accurate hit picking from multiple data sets important for efficient drug discovery. Here, we describe a screen design and data analysis approach that allow for normalization not only between quadrants and plates but also between screens or batches in a robust, quantitative fashion, enabling hit selection from multiple data sets. We independently screened the MicroSource Spectrum and NCI Diversity Set II libraries using a cell-based phenotypic high-through

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Falk, Shaun P., Andrew T. Ulijasz, and Bernard Weisblum. "Differential Assay for High-Throughput Screening of Antibacterial Compounds." Journal of Biomolecular Screening 12, no. 8 (2007): 1102–8. http://dx.doi.org/10.1177/1087057107308161.

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The previously described Bacillus subtilis reporter strain BAU-102 is capable of detecting cell wall synthesis inhibitors that act at all stages of the cell wall synthesis pathway. In addition, this strain is capable of detecting compounds with hydrophobic/ surfactant activity and alternative mechanisms of cell wall disruption. BAU-102 sequesters preformed β-gal in the periplasm, suggesting leakage of β-gal as the means by which this assay detects compound activities. A model is proposed according to which β-gal release by BAU-102 reflects activation of pathways leading to autolysis. The autho

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Kondo, Mitsuyo, Makiko Kawamoto, Atsushi Hasuoka, Masahiro Kajino, Nobuhiro Inatomi, and Naoki Tarui. "High-Throughput Screening of Potassium-Competitive Acid Blockers." Journal of Biomolecular Screening 17, no. 2 (2011): 177–82. http://dx.doi.org/10.1177/1087057111421004.

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H+,K+-ATPase is a key enzyme in the process of gastric acid secretion, and proton pump inhibitors (PPIs) have been accepted as one of the most effective treatments for peptic ulcer and gastroesophageal reflux disease. To discover a novel class of PPIs, the authors screened a low-molecular-weight compound library and identified two prospective acid blockers that were pyrrole derivatives. Both compounds inhibited H+,K+-ATPase in a reversible and potassium-competitive manner. These compounds led to the development of TAK-438 (1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methyl

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Schmid, Ingrid, Isabel Sattler, Susanne Grabley, and Ralf Thiericke. "Natural Products in High Throughput Screening: Automated High-Quality Sample Preparation." Journal of Biomolecular Screening 4, no. 1 (1999): 15–25. http://dx.doi.org/10.1177/108705719900400104.

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At present, compound libraries from combinatorial chemistry are the major source for high throughput screening (HTS) programs in drug discovery. On the other hand, nature has been proven to be an outstanding source for new and innovative drugs. Secondary metabolites from plants, animals, and microorganisms show a striking structural diversity that supplements chemically synthesized compounds or libraries in drug discovery programs. Unfortunately, extracts from natural sources are usually complex mixtures of compounds, often generated in time-consuming and, for the most part, manual processes.

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10

Xia, Menghang, Ruili Huang, Kristine L. Witt, et al. "Compound Cytotoxicity Profiling Using Quantitative High-Throughput Screening." Environmental Health Perspectives 116, no. 3 (2008): 284–91. http://dx.doi.org/10.1289/ehp.10727.

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11

Honma, Masaru, Mark Stubbs, Ian Collins, Paul Workman, Wynne Aherne, and Fiona M. Watt. "Identification of Novel Keratinocyte Differentiation Modulating Compounds by High-Throughput Screening." Journal of Biomolecular Screening 11, no. 8 (2006): 977–84. http://dx.doi.org/10.1177/1087057106292556.

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The authors have designed high-throughput screens to identify compounds that promote or inhibit terminal differentiation of primary human epidermal keratinocytes. Eleven known inhibitors of signaling pathways and approximately 4000 compounds of diverse structure were screened using an In-Cell Western system based on immunofluorescent staining of the terminal differentiation marker, involucrin. Staurosporine, a nonspecific protein kinase C inhibitor, and H89, a protein kinase A inhibitor, promoted expression of involucrin. Conversely, U0126, a MEK inhibitor, and SAHA or SBHA, 2 histone deacetyl

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Engels, Michael F. M., Luc Wouters, Rudi Verbeeck, and Greet Vanhoof. "Outlier Mining in High Throughput Screening Experiments." Journal of Biomolecular Screening 7, no. 4 (2002): 341–51. http://dx.doi.org/10.1177/108705710200700406.

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A data mining procedure for the rapid scoring of high-throughput screening (HTS) compounds is presented. The method is particularly useful for monitoring the quality of HTS data and tracking outliers in automated pharmaceutical or agrochemical screening, thus providing more complete and thorough structure-activity relationship (SAR) information. The method is based on the utilization of the assumed relationship between the structure of the screened compounds and the biological activity on a given screen expressed on a binary scale. By means of a data mining method, a SAR description of the dat

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Parham, Fred, Chris Austin, Noel Southall, Ruili Huang, Raymond Tice, and Christopher Portier. "Dose-Response Modeling of High-Throughput Screening Data." Journal of Biomolecular Screening 14, no. 10 (2009): 1216–27. http://dx.doi.org/10.1177/1087057109349355.

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The National Toxicology Program is developing a high-throughput screening (HTS) program to set testing priorities for compounds of interest, to identify mechanisms of action, and potentially to develop predictive models for human toxicity. This program will generate extensive data on the activity of large numbers of chemicals in a wide variety of biochemical- and cell-based assays. The first step in relating patterns of response among batteries of HTS assays to in vivo toxicity is to distinguish between positive and negative compounds in individual assays. Here, the authors report on a statist

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14

Forbes, Chris D., Joshuaine G. Toth, Can C. Özbal, et al. "High-Throughput Mass Spectrometry Screening for Inhibitors of Phosphatidylserine Decarboxylase." Journal of Biomolecular Screening 12, no. 5 (2007): 628–34. http://dx.doi.org/10.1177/1087057107301320.

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A high-throughput mass spectrometry assay to measure the catalytic activity of phosphatidylserine decarboxylase (PISD) is described. PISD converts phosphatidylserine to phosphatidylethanolamine during lipid synthesis. Traditional methods of measuring PISD activity are low throughput and unsuitable for the high-throughput screening of large compound libraries. The high-throughput mass spectrometry assay directly measures phosphatidylserine and phosphatidylethanolamine using the RapidFire™ platform at a rate of 1 sample every 7.5 s. The assay is robust, with an average Z′ value of 0.79 from a sc

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15

Benson, Neil, Helen F. Boyd, Jeremy R. Everett, et al. "NanoStore: A Concept for Logistical Improvements of Compound Handling in High-Throughput Screening." Journal of Biomolecular Screening 10, no. 6 (2005): 573–80. http://dx.doi.org/10.1177/1087057105277234.

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Small molecule screening, the systematic encounter of biology space with chemical space, has provoked the emergence of a whole industry that recreates itself by constant iterative improvements to this process. The authors describe an approach to tackle the problem for one of the most time-consuming steps in the execution of a screening campaign, namely, the reformatting of high-throughput screening test compounds from master plates to daughter assay plates used in the execution of the screen. Through an engineered storage procedure, they prepare plates ahead of the screening process with the r

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16

MORGAN, R. E., and N. J. WESTWOOD. "Screening and synthesis: high throughput technologies applied to parasitology." Parasitology 128, S1 (2004): S71—S79. http://dx.doi.org/10.1017/s0031182004007073.

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High throughput technologies continue to develop in response to the challenges set by the genome projects. This article discusses how the techniques of both high throughput screening (HTS) and synthesis can influence research in parasitology. Examples of the use of targeted and phenotype-based HTS using unbiased compound collections are provided. The important issue of identifying the protein target(s) of bioactive compounds is discussed from the synthetic chemist's perspective. This article concludes by reviewing recent examples of successful target identification studies in parasitology.

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Glick, Meir, Anthony E. Klon, Pierre Acklin, and John W. Davies. "Enrichment of Extremely Noisy High-Throughput Screening Data Using a Naïve Bayes Classifier." Journal of Biomolecular Screening 9, no. 1 (2004): 32–36. http://dx.doi.org/10.1177/1087057103260590.

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The noise level of a high-throughput screening (HTS) experiment depends on various factors such as the quality and robustness of the assay itself and the quality of the robotic platform. Screening of compound mixtures is noisier than screening single compounds per well. A classification model based on naïve Bayes (NB) may be used to enrich such data. The authors studied the ability of the NB classifier to prioritize noisy primary HTS data of compound mixtures (5 compounds/well) in 4 campaigns in which the percentage of noise presumed to be inactive compounds ranged between 81% and 91%. The top

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18

Sui, Shuo, Anne Mulichak, Raviraj Kulathila, et al. "A capillary-based microfluidic device enables primary high-throughput room-temperature crystallographic screening." Journal of Applied Crystallography 54, no. 4 (2021): 1034–46. http://dx.doi.org/10.1107/s1600576721004155.

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A novel capillary-based microfluidic strategy to accelerate the process of small-molecule-compound screening by room-temperature X-ray crystallography using protein crystals is reported. The ultra-thin microfluidic devices are composed of a UV-curable polymer, patterned by cleanroom photolithography, and have nine capillary channels per chip. The chip was designed for ease of sample manipulation, sample stability and minimal X-ray background. 3D-printed frames and cassettes conforming to SBS standards are used to house the capillary chips, providing additional mechanical stability and compatib

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19

Davies, Gareth, Hannah Semple, Megan McCandless, Jonathan Cairns, and Geoffrey A. Holdgate. "High-Throughput Mechanism of Inhibition." SLAS DISCOVERY: Advancing the Science of Drug Discovery 26, no. 2 (2021): 248–56. http://dx.doi.org/10.1177/2472555220983809.

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Enzymes represent a significant proportion of the druggable genome and constitute a rich source of drug targets. Delivery of a successful program for developing a modulator of enzyme activity requires an understanding of the enzyme’s mechanism and the mode of interaction of compounds. This allows an understanding of how physiological conditions in disease-relevant cells will affect inhibitor potency. As a result, there is increasing interest in evaluating hit compounds from high-throughput screens to determine their mode of interaction with the target. This work revisits the common inhibition

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20

Moriev, R., O. Vasylchenko, M. Platonov, O. Grygorenko, K. Volkova, and S. Zozulya. "Identification of Novel IGF1R Kinase Inhibitors by Molecular Modeling and High-Throughput Screening." Acta Naturae 5, no. 2 (2013): 90–99. http://dx.doi.org/10.32607/20758251-2013-5-2-90-99.

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The aim of this study was to identify small molecule compounds that inhibit the kinase activity of the IGF1 receptor and represent novel chemical scaffolds, which can be potentially exploited to develop drug candidates that are superior to the existing experimental anti-IGF1R therapeuticals. To this end, targeted compound libraries were produced by virtual screening using molecular modeling and docking strategies, as well as the ligand-based pharmacophore model. High-throughput screening of the resulting compound sets in a biochemical kinase inhibition assay allowed us to identify several nove

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21

Baugh, Chris, Shaohui Wang, Bin Li, James R. Appleman, and Peggy A. Thompson. "SCAN ™—A High-Throughput Assay for Detecting Small Molecule Binding to RNA Targets." Journal of Biomolecular Screening 14, no. 3 (2009): 219–29. http://dx.doi.org/10.1177/1087057108330111.

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A novel optical-based high-throughput screening technology has been developed for increasing the rate of discovering chemical leads against RNA targets. SCAN™ ( Screen for Compounds with Affinity for Nucleic Acids) is an affinity-based assay that identifies small molecules that bind and recognize structured RNA elements. This technology provides the opportunity to conduct high-throughput screening of a new class of targets—RNA. SCAN™ offers many attractive features including a simple homogeneous format, low screening costs, and the ability to use common laboratory equipment. A SCAN™ assay was

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22

Gergely, Szabolcs, Csaba Hegedűs, Petra Lakatos, et al. "High Throughput Screening Identifies a Novel Compound Protecting Cardiomyocytes from Doxorubicin-Induced Damage." Oxidative Medicine and Cellular Longevity 2015 (2015): 1–12. http://dx.doi.org/10.1155/2015/178513.

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Antracyclines are effective antitumor agents. One of the most commonly used antracyclines is doxorubicin, which can be successfully used to treat a diverse spectrum of tumors. Application of these drugs is limited by their cardiotoxic effect, which is determined by a lifetime cumulative dose. We set out to identify by high throughput screening cardioprotective compounds protecting cardiomyocytes from doxorubicin-induced injury. Ten thousand compounds of ChemBridge’s DIVERSet compound library were screened to identify compounds that can protect H9C2 rat cardiomyocytes against doxorubicin-induce

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MacGregor, Paula, Alasdair Ivens, Steven Shave, et al. "High-Throughput Chemical Screening for Antivirulence Developmental Phenotypes in Trypanosoma brucei." Eukaryotic Cell 13, no. 3 (2014): 412–26. http://dx.doi.org/10.1128/ec.00335-13.

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ABSTRACT In the bloodstream of mammalian hosts, the sleeping sickness parasite, Trypanosoma brucei , exists as a proliferative slender form or a nonproliferative, transmissible, stumpy form. The transition between these developmental forms is controlled by a density-dependent mechanism that is important for the parasite's infection dynamics, immune evasion via ordered antigenic variation, and disease transmissibility. However, stumpy formation has been lost in most laboratory-adapted trypanosome lines, generating monomorphic parasites that proliferate uncontrolled as slender forms in vitro and

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Gubler, Hanspeter, Ulrich Schopfer, and Edgar Jacoby. "Theoretical and Experimental Relationships between Percent Inhibition and IC50 Data Observed in High-Throughput Screening." Journal of Biomolecular Screening 18, no. 1 (2012): 1–13. http://dx.doi.org/10.1177/1087057112455219.

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The four-parameter logistic Hill equation models the theoretical relationship between inhibitor concentration and response and is used to derive IC50 values as a measure of compound potency. This relationship is the basis for screening strategies that first measure percent inhibition at a single, uniform concentration and then determine IC50 values for compounds above a threshold. In screening practice, however, a “good” correlation between percent inhibition values and IC50 values is not always observed, and in the literature, there seems confusion about what correlation even to expect. We ex

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Beggs, Mark. "Use of a Two-Armed Zymark(r) Robot for High Throughput Screening." Journal of Biomolecular Screening 2, no. 2 (1997): 71–78. http://dx.doi.org/10.1177/108705719700200204.

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High throughput screening is a key component of the pharmaceutical lead identification process at ZENECA. Robotic systems have been employed throughout the industry to perform (i) both the initial compound dilution and distribution processes that form a common "front end" to many high throughput screens and (ii) the assay assembly and signal detection steps that comprise an individual screen. Although the use of manipulative arm systems in formulating and replicating test compounds is well established, robotic throughput rates have been significantly slower than those that can be maintained by

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Tatman, Philip D., Tadeusz H. Wroblewski, Anthony R. Fringuello, et al. "High-Throughput Mechanistic Screening of Epigenetic Compounds for the Potential Treatment of Meningiomas." Journal of Clinical Medicine 10, no. 14 (2021): 3150. http://dx.doi.org/10.3390/jcm10143150.

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Background: Meningiomas are the most common primary central nervous system tumors. 20–30% of these tumors are considered high-grade and associated with poor prognosis and high recurrence rates. Despite the high occurrence of meningiomas, there are no FDA-approved compounds for the treatment of these tumors. Methods: In this study, we screened patient-cultured meningiomas with an epigenetic compound library to identify targetable mechanisms for the potential treatment of these tumors. Meningioma cell cultures were generated directly from surgically resected patient tumors and were cultured on a

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Nissink, J. Willem M., Stefan Schmitt, Sam Blackburn, and Stephen Peters. "Stratified High-Throughput Screening Sets Enable Flexible Screening Strategies from a Single Plated Collection." Journal of Biomolecular Screening 19, no. 3 (2013): 369–78. http://dx.doi.org/10.1177/1087057113498933.

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Customized compound picking and plating of very large corporate screening decks (many 100,000s) for high-throughput screening is generally restricted, both from a time and cost perspective. Here we present a stratified screening deck with accompanying plating design for use with very large corporate compound collections. The deck is plated as a whole, but copies for screening can be downsized flexibly and quickly on the fly, without the need for repicking of physical samples. We show that such downsized sets maximize returns and yield results superior to randomly picked subsets of the same siz

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Oprea, Tudor I., Cristian G. Bologa, Bruce S. Edwards, Eric R. Prossnitz, and Larry A. Sklar. "Post-High-Throughput Screening Analysis: An Empirical Compound Prioritization Scheme." Journal of Biomolecular Screening 10, no. 5 (2005): 419–26. http://dx.doi.org/10.1177/1087057104272660.

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An empirical scheme to evaluate and prioritize screening hits from high-throughput screening (HTS) is proposed. Negative scores are given when chemotypes found in the HTS hits are present in annotated databases such as MDDR and WOMBAT or for testing positive in toxicity-related experiments reported in TOXNET. Positive scores were given for higher measured biological activities, for testing negative in toxicity-related literature, and for good overlap when profiled against drug-related properties. Particular emphasis is placed on estimating aqueous solubility to prioritize in vivo experiments.

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LI, MIN. "High-Throughput Compound Screening and Discovery in an Academic Setting." Retina 25, Supplement (2005): S58—S59. http://dx.doi.org/10.1097/00006982-200512001-00026.

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Zander Balderud, Linda, David Murray, Niklas Larsson, et al. "Using the BioAssay Ontology for Analyzing High-Throughput Screening Data." Journal of Biomolecular Screening 20, no. 3 (2014): 402–15. http://dx.doi.org/10.1177/1087057114563493.

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High-throughput screening (HTS) is the main starting point for hit identification in drug discovery programs. This has led to a rapid increase of available screening data both within pharmaceutical companies and the public domain. We have used the BioAssay Ontology (BAO) 2.0 for assay annotation within AstraZeneca to enable comparison with external HTS methods. The annotated assays have been analyzed to identify technology gaps, evaluate new methods, verify active hits, and compare compound activity between in-house and PubChem assays. As an example, the binding of a fluorescent ligand to form

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Prummer, Michael. "Hypothesis Testing in High-Throughput Screening for Drug Discovery." Journal of Biomolecular Screening 17, no. 4 (2012): 519–29. http://dx.doi.org/10.1177/1087057111431278.

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Following the success of small-molecule high-throughput screening (HTS) in drug discovery, other large-scale screening techniques are currently revolutionizing the biological sciences. Powerful new statistical tools have been developed to analyze the vast amounts of data in DNA chip studies, but have not yet found their way into compound screening. In HTS, characterization of single-point hit lists is often done only in retrospect after the results of confirmation experiments are available. However, for prioritization, for optimal use of resources, for quality control, and for comparison of sc

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Adachi, Ryutaro, Tsuyoshi Ishii, Shinichi Matsumoto, Takuya Satou, Junichi Sakamoto, and Tomohiro Kawamoto. "Discovery of Human Intestinal MGAT Inhibitors Using High-Throughput Mass Spectrometry." SLAS DISCOVERY: Advancing the Science of Drug Discovery 22, no. 4 (2016): 360–65. http://dx.doi.org/10.1177/1087057116673181.

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Monoacylglycerol acyltransferase (MGAT) activity catalyzes the synthesis of diacylglycerol (DAG) from fatty acyl-CoA and monoacylglycerol as substrates. It is important for the resynthesis of triacylglycerol (TAG) in the intestine. In the present study, we developed a MGAT enzymatic assay of human intestinal microsomes using a high-throughput mass spectrometry (MS)–based detection system. After screening with small-molecular-weight libraries for compounds exhibiting inhibitions against DAG and the consequent TAG syntheses, we identified multiple compounds that specifically inhibit intestinal M

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Anderson, Steven N., Danli L. Towne, David J. Burns, and Usha Warrior. "A High-Throughput Soft Agar Assay for Identification of Anticancer Compound." Journal of Biomolecular Screening 12, no. 7 (2007): 938–45. http://dx.doi.org/10.1177/1087057107306130.

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A 384-well soft agar assay was developed to identify potential novel anticancer compounds. Normally used to detect cell transformation, the assay is used here to quantitate cell proliferation in a 3-dimensional (3-D) anchorage-independent format. HCC827 cells, which are highly sensitive to epithelial growth factor receptor (EGFR) tyrosine kinase inhibitors, were used to develop the method and a set of 9600 compounds used to validate the assay. Results were compared to a monolayer assay using the same compound set. The assay provides a robust method to discover compounds that could be missed us

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Ricci, F., L. Carrassa, M. S. Christodoulou, et al. "A High-throughput Screening of a Chemical Compound Library in Ovarian Cancer Stem Cells." Combinatorial Chemistry & High Throughput Screening 21, no. 1 (2018): 50–56. http://dx.doi.org/10.2174/1386207321666180124093406.

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Background: Epithelial ovarian cancer has a poor prognosis, mostly due to its late diagnosis and the development of drug resistance after a first platinum-based regimen. The presence of a specific population of “cancer stem cells” could be responsible of the relapse of the tumor and the development of resistance to therapy. For this reason, it would be important to specifically target this subpopulation of tumor cells in order to increase the response to therapy. Method: We screened a chemical compound library assembled during the COST CM1106 action to search for compound classes active in tar

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Xu, Danqing, Zhiheng Xu, Li Han, et al. "Identification of New ATG4B Inhibitors Based on a Novel High-Throughput Screening Platform." SLAS DISCOVERY: Advancing the Science of Drug Discovery 22, no. 4 (2016): 338–47. http://dx.doi.org/10.1177/1087057116639202.

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Autophagy is an evolutionarily conserved homeostasis process through which aggregated proteins or damaged organelles are enveloped in a double-membrane structure called an autophagosome and then digested in a lysosome-dependent manner. Growing evidence suggests that malfunction of autophagy contributes to the pathogenesis of a variety of diseases, including cancer, viral infection, and neurodegeneration. However, autophagy is a complicated process, and understanding of the relevance of autophagy to disease is limited by lack of specific and potent autophagy modulators. ATG4B, a Cys-protease th

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Terry-Lorenzo, Ryan T., Keiki Masuda, Kohtaroh Sugao, et al. "High-Throughput Screening Strategy Identifies Allosteric, Covalent Human D-Amino Acid Oxidase Inhibitor." Journal of Biomolecular Screening 20, no. 10 (2015): 1218–31. http://dx.doi.org/10.1177/1087057115600413.

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Genome-wide association studies have linked polymorphisms in the gene G72 to schizophrenia risk in several human populations. Although controversial, biochemical experiments have suggested that the mechanistic link of G72 to schizophrenia is due to the G72 protein product, pLG72, exerting a regulatory effect on human D-amino acid oxidase (hDAAO) activity. In an effort to identify hDAAO inhibitors of novel mechanism of action, we designed a pLG72-directed hDAAO activity assay suitable for high-throughput screening (HTS). During assay development, we confirmed that pLG72 was an inhibitor of hDAA

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Severson, William E., Michael McDowell, Subramaniam Ananthan, et al. "High-Throughput Screening of a 100,000-Compound Library for Inhibitors of Influenza A Virus (H3N2)." Journal of Biomolecular Screening 13, no. 9 (2008): 879–87. http://dx.doi.org/10.1177/1087057108323123.

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Using a highly reproducible and robust cell-based high-throughput screening (HTS) assay, the authors screened a 100,000-compound library at 14- and 114-µM compound concentration against influenza strain A/Udorn/72 (H3N2). The “hit” rates (>50% inhibition of the viral cytopathic effect) from the 14- and 114-µM screens were 0.022% and 0.38%, respectively. The hits were evaluated for their antiviral activity, cell toxicity, and selectivity in dose-response experiments. The screen at the lower concentration yielded 3 compounds, which displayed moderate activity (SI50 = 10-49). Intriguingly, the

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Coma, Isabel, Liz Clark, Emilio Diez, et al. "Process Validation and Screen Reproducibility in High-Throughput Screening." Journal of Biomolecular Screening 14, no. 1 (2008): 66–76. http://dx.doi.org/10.1177/1087057108326664.

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The use of large-scale compound screening has become a key component of drug discovery projects in both the pharmaceutical and the biotechnological industries. More recently, these activities have also been embraced by the academic community as a major tool for chemical genomic activities. High-throughput screening (HTS) activities constitute a major step in the initial drug discovery efforts and involve the use of large quantities of biological reagents, hundreds of thousands to millions of compounds, and the utilization of expensive equipment. All these factors make it very important to eval

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Moger, Julian, Philip Gribbon, Andreas Sewing, and C. Peter Winlove. "The Application of Fluorescence Lifetime Readouts in High-Throughput Screening." Journal of Biomolecular Screening 11, no. 7 (2006): 765–72. http://dx.doi.org/10.1177/1087057106291541.

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Measurement of fluorescence lifetime is a well-established technique, which has recently been introduced into the portfolio of assay formats used in high-throughput screening (HTS). This investigation establishes appropriate conditions for using lifetime measurements to reduce the impact of compound interference effects during large-scale HTS of corporate screening files. Experimental data on mixtures of standard fluorophores and interfering compounds (from 5 HTS campaigns) have been combined with a theoretical model to identify the minimum data quality required, defined by the photon count in

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Gribbon, Philip, Chris Chambers, Kaupo Palo, Juergen Kupper, Juergen Mueller, and Andreas Sewing. "A Novel Method for Analyzing [Ca2+] Flux Kinetics in High-Throughput Screening." Journal of Biomolecular Screening 11, no. 5 (2006): 511–18. http://dx.doi.org/10.1177/1087057106287929.

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Driven by multiparameter fluorescence readouts and the analysis of kinetic responses from biological assay systems, the amount and complexity of high-throughput screening data are constantly increasing. As a consequence, the reduction of data to a simple number, reflecting a percentage activity/inhibition, is no longer an adequate approach because valuable additional information, for example, about compound-or process-induced artifacts, is lost. Time series data such as the transient calcium flux observed after activation of Gq-coupled G protein-coupled receptors (GPCRs), are especially challe

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Young, Susan M., Mark S. Curry, John T. Ransom, et al. "High-Throughput Microfluidic Mixing and Multiparametric Cell Sorting for Bioactive Compound Screening." Journal of Biomolecular Screening 9, no. 2 (2004): 103–11. http://dx.doi.org/10.1177/1087057103262335.

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HyperCyt®, an automated sample handling system for flow cytometry that uses air bubbles to separate samples sequentially introduced from multiwell plates by an autosampler. In a previously documented HyperCyt® configuration, air bubble separated compounds in one sample line and a continuous stream of cells in another are mixed in-line for serial flow cytometric cell response analysis. To expand capabilities for high-throughput bioactive compound screening, the authors investigated using this system configuration in combination with automated cell sorting. Peptide ligands were sampled from a 96

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Tawa, Paul, Jean-Pierre Falgueyret, Sebastien Guiral, et al. "High-Throughput Scintillation Proximity Assay for Stearoyl-CoA Desaturase-1." Journal of Biomolecular Screening 16, no. 5 (2011): 506–17. http://dx.doi.org/10.1177/1087057111399436.

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Stearoyl-CoA desaturase (SCD) catalyzes the synthesis of monounsaturated fatty acids and has been implicated in a number of disease states, including obesity and diabetes. To find small-molecule inhibitor leads, a high-throughput scintillation proximity assay (SPA) was developed using the hydrophobic binding characteristics of a glass microsphere scintillant bead to capture SCD1 from a crude lysate of recombinant SCD1 in Sf9 lysate coupled with the strong binding characteristics of an azetidine compound ([3H]AZE). The SPA assay was stable over 24 h and could detect compounds with micromolar to

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Elkin, L. L., D. G. Harden, S. Saldanha, et al. "Just-in-Time Compound Pooling Increases Primary Screening Capacity without Compromising Screening Quality." Journal of Biomolecular Screening 20, no. 5 (2015): 577–87. http://dx.doi.org/10.1177/1087057115572988.

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Compound pooling, or multiplexing more than one compound per well during primary high-throughput screening (HTS), is a controversial approach with a long history of limited success. Many issues with this approach likely arise from long-term storage of library plates containing complex mixtures of compounds at high concentrations. Due to the historical difficulties with using multiplexed library plates, primary HTS often uses a one-compound–one-well approach. However, as compound collections grow, innovative strategies are required to increase the capacity of primary screening campaigns. Toward

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FAGHIRI, Z., R. BONILLA SANTIAGO, Z. WU, and G. WIDMER. "High-throughput screening in suboptimal growth conditions identifies agonists ofGiardia lambliaproliferation." Parasitology 138, no. 2 (2010): 194–200. http://dx.doi.org/10.1017/s0031182010001101.

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SUMMARYGiardia lambliais one of the most prevalent parasites of mankind and is estimated to cause over 200 million infections per year. To screen chemical libraries for compounds that perturb trophozoite proliferation we adapted a conventional culture method to 384-well plates and identified numerous inhibitors. Here we used a modified assay to screen for compounds that promote trophozoite multiplication. Trophozoite growth was reduced by dilution of the culture medium and the growth period was extended to screen 2 compound libraries comprising 1500 compounds. A total of 4 agonists of trophozo

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Ravi D, Chaitanya Kumar K, Mothilal K, and Mahender K. "High throughput virtual screening of cyclooxygenase-2 by using database." International Journal of Pharmaceutical Research and Life Sciences 8, no. 2 (2020): 97–100. http://dx.doi.org/10.26452/ijprls.v8i2.1358.

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COX-2 is a type of Non-steroidal mitigating drug (NSAID) that legitimately targets COX-2, a protein liable for irritation and torment. Selectivity for COX-2 decreases the danger of peptic ulceration and is the fundamental component of celecoxib, rofecoxib and different individuals from this medication class. COX-2 selectivity doesn't appear to influence other antagonistic impacts of NSAIDs (most prominently an expanded danger of renal disappointment), and a few outcomes have excited the doubt that there may be an expansion in danger for cardiovascular failure, apoplexy and stroke by a relative

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Brideau, Christine, Bert Gunter, Bill Pikounis, and Andy Liaw. "Improved Statistical Methods for Hit Selection in High-Throughput Screening." Journal of Biomolecular Screening 8, no. 6 (2003): 634–47. http://dx.doi.org/10.1177/1087057103258285.

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High-throughput screening (HTS) plays a central role in modern drug discovery, allowing the rapid screening of large compound collections against a variety of putative drug targets. HTS is an industrial-scale process, relying on sophisticated auto mation, control, and state-of-the art detection technologies to organize, test, and measure hundreds of thousands to millions of compounds in nano-to microliter volumes. Despite this high technology, hit selection for HTS is still typically done using simple data analysis and basic statistical methods. The authors discuss in this article some shortco

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Li, Xue, Jun Yang, Xiaobo He, et al. "Identification of Upregulators of BMP2 Expression via High-Throughput Screening of a Synthetic and Natural Compound Library." Journal of Biomolecular Screening 14, no. 10 (2009): 1251–56. http://dx.doi.org/10.1177/1087057109346446.

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Bone morphogenetic protein II (BMP2), a member of the transforming growth factor—β (TGF-β) superfamily, is highly expressed in osteoblasts and is a crucial regulator of osteogenic differentiation . Many observations clearly indicate the high potency of BMP2 as an inducer of osteogenesis, and it may be a novel therapeutic target for diseases associated with bone loss, especially in menopausal and postmenopausal women. To discover new agents that enhance the expression of the mouse BMP2, the authors developed a high-throughput assay to screen a synthetic and natural compound library. The cell-ba

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Shu, Chih-Wen, Charitha Madiraju, Dayong Zhai, et al. "High-Throughput Fluorescence Assay for Small-Molecule Inhibitors of Autophagins/Atg4." Journal of Biomolecular Screening 16, no. 2 (2011): 174–82. http://dx.doi.org/10.1177/1087057110392996.

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Autophagy is an evolutionarily conserved process for catabolizing damaged proteins and organelles in a lysosome-dependent manner. Dysregulation of autophagy may cause various diseases, such as cancer and neurodegeneration. However, the relevance of autophagy to diseases remains controversial because of the limited availability of chemical modulators. Herein, the authors developed a fluorescence-based assay for measuring activity of the autophagy protease, autophagin-1(Atg4B). The assay employs a novel reporter substrate of Atg4B composed of a natural substrate (LC3B) fused to an assayable enzy

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Ordas, Anita, Robert-Jan Raterink, Fraser Cunningham, et al. "Testing Tuberculosis Drug Efficacy in a Zebrafish High-Throughput Translational Medicine Screen." Antimicrobial Agents and Chemotherapy 59, no. 2 (2014): 753–62. http://dx.doi.org/10.1128/aac.03588-14.

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ABSTRACTThe translational value of zebrafish high-throughput screens can be improved when more knowledge is available on uptake characteristics of potential drugs. We investigated reference antibiotics and 15 preclinical compounds in a translational zebrafish-rodent screening system for tuberculosis. As a major advance, we have developed a new tool for testing drug uptake in the zebrafish model. This is important, because despite the many applications of assessing drug efficacy in zebrafish research, the current methods for measuring uptake using mass spectrometry do not take into account the

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Young, Susan M., Cristian Bologa, Eric R. Prossnitz, Tudor I. Oprea, Larry A. Sklar, and Bruce S. Edwards. "High-Throughput Screening with HyperCyt® Flow Cytometry to Detect Small Molecule Formylpeptide Receptor Ligands." Journal of Biomolecular Screening 10, no. 4 (2005): 374–82. http://dx.doi.org/10.1177/1087057105274532.

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High-throughput flow cytometry (HTFC), enabled by faster automated sample processing, represents a promising high- content approach for compound library screening. HyperCyt® is a recently developed automated HTFC analysis system by which cell samples are rapidly aspirated from microplate wells and delivered to the flow cytometer. The formylpeptide receptor (FPR) family of G protein–coupled receptors contributes to the localization and activation of tissue-damaging leukocytes at sites of chronic inflammation. Here, the authors describe development and application of an HTFC screening approach t

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