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Assay and Drug Development Technologies

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https://www.readbyqxmd.com/read/29608094/utility-of-resazurin-horseradish-peroxidase-and-nmr-assays-to-identify-redox-related-false-positive-behavior-in-high-throughput-screens
#1
Matthew Tarnowski, Amélie Barozet, Carina Johansson, Per-Olof Eriksson, Ola Engkvist, Jarrod Walsh, J Willem M Nissink
Discerning false positives from true actives in high-throughput screening (HTS) output is fraught with difficulty as the reason of anomalous activity seen for compounds is often not clear-cut. In this study, we introduce a novel medium-throughput NMR assay for the identification of redox-cycling compounds (RCCs), which is based on detection of oxidation of a reducing agent. We compare its outcomes to those from horseradish peroxidase (HRP)/phenol red and resazurin (RZ)-based assays that are more commonly used for triaging HTS outputs...
April 2, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29658791/high-throughput-gene-expression-profiles-to-define-drug-similarity-and-predict-compound-activity
#2
Hans De Wolf, Laure Cougnaud, Kirsten Van Hoorde, An De Bondt, Joerg K Wegner, Hugo Ceulemans, Hinrich Göhlmann
By adding biological information, beyond the chemical properties and desired effect of a compound, uncharted compound areas and connections can be explored. In this study, we add transcriptional information for 31K compounds of Janssen's primary screening deck, using the HT L1000 platform and assess (a) the transcriptional connection score for generating compound similarities, (b) machine learning algorithms for generating target activity predictions, and (c) the scaffold hopping potential of the resulting hits...
April 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29658790/a-high-throughput-time-resolved-fluorescence-energy-transfer-assay-to-screen-for-modulators-of-rgs7-g%C3%AE-5-r7bp-complex
#3
Brian S Muntean, Dipak N Patil, Franck Madoux, James Fossetta, Louis Scampavia, Timothy P Spicer, Kirill A Martemyanov
G protein-coupled receptors (GPCRs) are excellent drug targets exploited by majority of the Food and Drug Administration-approved medications, but when modulated, are often accompanied by significant adverse effects. Targeting of other elements in GPCR pathways for improved safety and efficacy is thus an unmet need. The strength of GPCR signaling is tightly regulated by regulators of G protein signaling (RGS) proteins, making them attractive drug targets. We focused on a prominent RGS complex in the brain consisting of RGS7 and its binding partners Gβ5 and R7BP...
April 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29658789/effect-of-2-phenylethanol-as-antifungal-agent-and-common-antifungals-amphotericin-b-fluconazole-and-itraconazole-on-candida-species-isolated-from-chronic-and-recurrent-cases-of-candidal-vulvovaginitis
#4
Niloufar Majdabadi, Mehraban Falahati, Fariba Heidarie-Kohan, Shirin Farahyar, Parvaneh Rahimi-Moghaddam, Mahtab Ashrafi-Khozani, Tandis Razavi, Sina Mohammadnejad
The antifungal effects of 2-phenylethanol are clearly visible through its intervention in Candida morphogenesis. Chronic and recurrent vulvovaginitis, however, does not respond to this standard experimental therapy; therefore, the study presented in this article investigated the effect of common antifungal drugs (amphotericin B [AMB], fluconazole [FLU], and itraconazole [ITC]), in combination with 2-phenylethanol, on the Candida species isolated from cases of chronic and recurrent vulvovaginitis, thereby allowing the recommendation of a more appropriate treatment option...
April 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29658788/literature-search-and-review
#5
Anton Simeonov, Aaron Wilson, Doug Auld
No abstract text is available yet for this article.
April 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29446984/anticancer-drugs-as-antibiofilm-agents-in-candida-albicans-potential-targets
#6
Archana Anandrao Wakharde, Shivkrupa Devrao Halbandge, Datta Baburao Phule, Sankunny Mohan Karuppayil
The human pathogen Candida albicans can grow as a biofilm on host tissues and on the surfaces of different prosthetic devices in a patient's body. Various studies have reported that biofilms formed by C. albicans are resistant to most of the currently used antibiotics including the widely prescribed drug, fluconazole. As such, novel strategies for the treatment of drug-resistant biofilms are required. Drug repositioning or the use of drugs outside their unique indication has the potential to radically change drug development...
February 15, 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29634317/development-of-a-time-resolved-fluorescence-resonance-energy-transfer-ultrahigh-throughput-screening-assay-for-targeting-the-nsd3-and-myc-interaction
#7
Jinglin Xiong, Valentina Gonzalez Pecchi, Min Qui, Andrey A Ivanov, Xiulei Mo, Qiankun Niu, Xiang Chen, Haian Fu, Yuhong Du
Epigenetic modulators play critical roles in reprogramming of cellular functions, emerging as a new class of promising therapeutic targets. Nuclear receptor binding SET domain protein 3 (NSD3) is a member of the lysine methyltransferase family. Interestingly, the short isoform of NSD3 without the methyltransferase fragment, NSD3S, exhibits oncogenic activity in a wide range of cancers. We recently showed that NSD3S interacts with MYC, a central regulator of tumorigenesis, suggesting a mechanism by which NSD3S regulates cell proliferation through engaging MYC...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29493258/development-of-a-neo-epitope-specific-assay-for-serological-assessment-of-type-vii-collagen-turnover-and-its-relevance-in-fibroproliferative-disorders
#8
Jannie M B Sand, Patricia Lamy, Pernille Juhl, Anne Sofie Siebuhr, Line V Iversen, Arkadiusz Nawrocki, Martin R Larsen, Robyn T Domsic, Nathalie Franchimont, Juan Chavez, Morten A Karsdal, Diana J Leeming
Type VII collagen is the main component of the anchoring fibrils connecting the basement membrane to the underlying interstitial matrix. Mutations in the type VII collagen gene cause dystrophic epidermolysis bullosa. Increased levels of type VII collagen in the skin have been reported in patients with systemic sclerosis (SSc), whereas reduced levels in the airways have been related to asthma. This indicates that type VII collagen plays an important part in upholding tissue integrity and that its remodeling may lead to pathological states...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29470101/ebselen-reversibly-inhibits-human-glutamate-dehydrogenase-at-the-catalytic-site
#9
Yanhong Jin, Di Li, Shiying Lu, Han Zhao, Zhao Chen, Wei Hou, Benfang Helen Ruan
Human glutamate dehydrogenase (GDH) plays an important role in neurological diseases, tumor metabolism, and hyperinsulinism-hyperammonemia syndrome (HHS). However, there are very few inhibitors known for human GDH. Recently, Ebselen was reported to crosslink with Escherichia coli GDH at the active site cysteine residue (Cys321), but the sequence alignment showed that the corresponding residue is Ala329 in human GDH. To investigate whether Ebselen could be an inhibitor for human GDH, we cloned and expressed an N-terminal His-tagged human GDH in E...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29469589/preparation-of-vitamin-e-containing-high-density-lipoprotein-and-its-protective-efficacy-on-macrophages
#10
Manman Su, Dingding Wang, Weiqin Chang, Lixian Liu, Manhua Cui, Tianmin Xu
Atherosclerosis is a major cause for cardiovascular diseases. High-density lipoprotein (HDL) may reduce atherosclerosis through several different mechanisms. HDL is composed of lipids, cholesterol, cholesteryl esters, triglycerides, and phospholipids, mainly phosphatidylcholine plus specialized proteins called apolipoproteins (apos). In this study, we prepared vitamin E containing HDL (VE -HDL) that contains egg phosphatidylcholine, cholesterol, vitamin E, and two kinds of recombinant human apolipoproteins (rhapo)-rhapoA-I and rhapoE in vitro by the facilitation of cholate...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29443535/literature-search-and-review
#11
Anton Simeonov, Aaron Wilson, Doug Auld
No abstract text is available yet for this article.
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29394094/integration-of-antibody-array-technology-into-drug-discovery-and-development
#12
Wei Huang, Kelly Whittaker, Huihua Zhang, Jian Wu, Si-Wei Zhu, Ruo-Pan Huang
Antibody arrays represent a high-throughput technique that enables the parallel detection of multiple proteins with minimal sample volume requirements. In recent years, antibody arrays have been widely used to identify new biomarkers for disease diagnosis or prognosis. Moreover, many academic research laboratories and commercial biotechnology companies are starting to apply antibody arrays in the field of drug discovery. In this review, some technical aspects of antibody array development and the various platforms currently available will be addressed; however, the main focus will be on the discussion of antibody array technologies and their applications in drug discovery...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29389222/2017-acknowledgment-of-reviewers
#13
(no author information available yet)
No abstract text is available yet for this article.
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29345980/society-of-biomolecular-imaging-and-informatics-high-content-screening-high-content-analysis-emerging-technologies-in-biological-models-when-and-why
#14
Ann F Hoffman, John Nolan, David F Gebhard, Debra Nickischer, Wienand Omta, Sam Cooper, Sharon Presnell, Judi Wardwell-Swanson, Myles Fennell
No abstract text is available yet for this article.
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29345979/machine-learning-enables-live-label-free-phenotypic-screening-in-three-dimensions
#15
Eoghan O'Duibhir, Jasmin Paris, Hannah Lawson, Catarina Sepulveda, Dahlia Doughty Shenton, Neil O Carragher, Kamil R Kranc
There is a large amount of information in brightfield images that was previously inaccessible by using traditional microscopy techniques. This information can now be exploited by using machine-learning approaches for both image segmentation and the classification of objects. We have combined these approaches with a label-free assay for growth and differentiation of leukemic colonies, to generate a novel platform for phenotypic drug discovery. Initially, a supervised machine-learning algorithm was used to identify in-focus colonies growing in a three-dimensional (3D) methylcellulose gel...
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29345978/research-in-rare-disease-from-genomics-to-proteomics
#16
Jessica Lacoste
Jessica Lacoste from the Donnelly Centre at the University of Toronto was awarded best poster at the annual Society of Biomolecular Imaging and Informatics meeting held in San Diego, September 2017. Her work focuses on characterizing the protein localization of variants involved in rare disease. The current works and future directions of research in rare disease are summarized in the following overview.
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29266960/flecs-technology-for-high-throughput-single-cell-force-biology-and-screening
#17
Ivan Pushkarsky
Dr. Ivan Pushkarsky from the Department of Bioengineering at UCLA and Forcyte Biotechnologies, Inc. was awarded The President's Innovation Award at the Annual Society of Biomolecular Imaging and Informatics meeting held in San Diego, September 2017. All cell types produce mechanical forces to serve important physiological roles. Since aberrant force-generating phenotypes directly lead to disease, cellular force-generation mechanisms are high-value targets for new therapies. Despite knowledge of their significance in disease, drug developers have had limited access to force-generating cellular phenotypes, especially in the context of high-throughput screening...
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29215913/high-content-screening-comparison-of-cancer-drug-accumulation-and-distribution-in-two-dimensional-and-three-dimensional-culture-models-of-head-and-neck-cancer
#18
Feng Shan, David A Close, Daniel P Camarco, Paul A Johnston
High cancer drug development attrition rates have provoked considerable debate about whether the two-dimensional tumor growth inhibition high-throughput screening assays used in pre-clinical lead discovery adequately reflect solid tumor complexity. We used automated high-content screening image acquisition and analysis methods to compare fluorescent drug uptake, accumulation, and distribution in Cal33 and FaDu head and neck cancer (HNC) monolayer and multicellular tumor spheroid (MCTS) models. Ellipticine, idarubicin, daunorubicin, and doxorubicin were studied because of their fluorescent properties and broad anti-tumor activities...
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29148820/a-functional-kinase-short-interfering-ribonucleic-acid-screen-using-protease-activated-receptor-2-dependent-opening-of-transient-receptor-potential-vanilloid-4
#19
William G Darby, Megan S Grace, Kaylene J Simpson, Owen L Woodman, Peter McIntyre
Protease-activated receptor 2 (PAR2 ) is a proinflammatory G-protein coupled receptor (GPCR) that is activated by inflammatory proteases, and its activation initiates signaling pathways that modulate the nonselective cation channel transient receptor potential vanilloid-4 (TRPV4). PAR2 -dependent opening of TRPV4 has been attributed to kinase activation, but the identity of the responsible enzymes is unknown. Deciphering the signaling pathways involved in the PAR2 -dependent opening of TRPV4 may yield new targets for pain treatment...
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28891675/abstracts-the-society-of-biomolecular-imaging-and-informatics-4th-annual-meeting-poster-session-september-13-15-2017-san-diego-convention-center-san-diego-ca
#20
(no author information available yet)
No abstract text is available yet for this article.
January 2018: Assay and Drug Development Technologies
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