HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus.

abstract：:Intracerebroventricular injection of angiotensin IV, a ligand of insulin-regulated aminopeptidase (IRAP), has been shown to improve cognitive functions in several animal models. Consequently, IRAP is considered a potential target for treatment of cognitive disorders. To identify nonpeptidic IRAP inhibitors, we adapted...

journal_title：Assay and drug development technologies

authors： Engen K,Rosenström U,Axelsson H,Konda V,Dahllund L,Otrocka M,Sigmundsson K,Nikolaou A,Vauquelin G,Hallberg M,Jenmalm Jensen A,Lundbäck T,Larhed M

更新日期：2016-04-01 00:00:00

abstract：:Coronavirus disease 2019 (COVID-19), caused by the SARS-CoV-2 virus, has developed into a pandemic causing major disruptions and hundreds of thousands of deaths in wide parts of the world. As of July 3, 2020, neither vaccines nor approved drugs for effective treatment are available. In this article, we showcase how to...

journal_title：Assay and drug development technologies

authors： Matschinske J,Salgado-Albarrán M,Sadegh S,Bongiovanni D,Baumbach J,Blumenthal DB

更新日期：2020-11-01 00:00:00

abstract：:Angiogenesis is a general term describing formation of new tube-like microvessel sprouts that are the size of capillary blood vessels. Angiogenesis is fundamental in key stages of embryonic development, organ formation, and wound repair and is also involved in the development and progression of a variety of pathologic...

journal_title：Assay and drug development technologies

authors： Santos AF,Zaltsman AB,Martin RC,Kuzmin A,Alexandrov Y,Roquemore EP,Jessop RA,van Erck MG,Verheijen JH

更新日期：2008-10-01 00:00:00

abstract：:Urinary tract infections (UTIs), including cystitis and pyelonephritis, affect a large proportion of the population and account for significant medical costs. In more than 80% of UTIs, uropathogenic Escherichia coli (UPEC) is the causative pathogen. The initial step in the pathogenesis of the infection is the adherenc...

journal_title：Assay and drug development technologies

authors： Scharenberg M,Abgottspon D,Cicek E,Jiang X,Schwardt O,Rabbani S,Ernst B

更新日期：2011-10-01 00:00:00

abstract：:Voltage-gated sodium (Na(V)) channels have an essential role in the initiation and propagation of action potentials in excitable cells, such as neurons. Of these channels, Na(V)1.7 has been indicated as a key channel for pain sensation. While extensive efforts have gone into discovering novel Na(V)1.7 modulating compo...

journal_title：Assay and drug development technologies

authors： Chambers C,Witton I,Adams C,Marrington L,Kammonen J

更新日期：2016-03-01 00:00:00

abstract：:Sphingosine kinases (SPHKs) catalyze the formation of the bioactive sphingolipid metabolite sphingosine 1-phosphate (S1P), which plays important roles in a wide variety of intra- and extracellular functions. Conventionally, SPHK activity has been determined using radioisotope thin layer chromatography (TLC) and autora...

journal_title：Assay and drug development technologies

authors： Togame H,Dodo R,Inaoka T,Reinemer P

更新日期：2007-04-01 00:00:00

abstract：:This study aimed to synthesize methoxy polyethylene glycol propionaldehyde (mPEG20,000-ALD) for the preparation of PEGylated nanoliposomal cisplatin. Nanocarriers such as liposomes are developed for a wide range of drug delivery systems. PEG with high molecular weight (Mw) is used to coat the liposomes. In this study,...

journal_title：Assay and drug development technologies

authors： Shirzad M,Jamehbozorgi S,Akbarzadeh I,Aghabozorg HR,Amini A

更新日期：2019-07-01 00:00:00

abstract：:Software, named Cardio Analyser, was developed for digital movie analysis of beating frequencies, drug-induced chronotropic effects, and quantification of beating areas of contracting cardiomyocyte cultures. A major novelty of the software is the introduction of automated noise filtering and automated movie analysis o...

journal_title：Assay and drug development technologies

authors： Stummann TC,Wronski M,Sobanski T,Kumpfmueller B,Hareng L,Bremer S,Whelan MP

更新日期：2008-06-01 00:00:00

abstract：: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 be...

journal_title：Assay and drug development technologies

authors： Darby WG,Grace MS,Simpson KJ,Woodman OL,McIntyre P

更新日期：2018-01-01 00:00:00

abstract：:Over the past decade, microarray technology has become a powerful tool to provide a genome-wide view of genetic or epigenetic changes associated with tumor metastasis. To extract biologically meaningful information from the vast amounts of microarray data, it is crucial to choose suitable biological systems and have v...

journal_title：Assay and drug development technologies

authors： Yang J

更新日期：2006-08-01 00:00:00

abstract：:Steroid receptors belong to the nuclear hormone receptor superfamily, which represents one of the important families of drug targets in the pharmaceutical industry. These receptors are generally expressed in a broad range of tissues and play roles in multiple physiological pathways. They represent one of the most comp...

journal_title：Assay and drug development technologies

authors： Bai C,Schmidt A,Freedman LP

更新日期：2003-12-01 00:00:00

abstract：:An atomic absorption spectroscopy-based detection system was employed to develop a new non-radioactive flux assay for chloride (Cl-) channels in a high throughput format. Cl- flux is assayed by measuring the extent to which Cl- precipitates an excess amount of silver ions (Ag+). A linear correlation was observed betwe...

journal_title：Assay and drug development technologies

authors： Gill S,Gill R,Xie Y,Wicks D,Liang D

更新日期：2006-02-01 00:00:00

abstract：:Reverse cholesterol transport is the process by which extrahepatic cells, including macrophage-derived foam cells in arterial atherosclerotic plaque, transport excessive cholesterol back to the liver for bile acid synthesis and excretion, thus lowering the peripheral lipid burden. Cholesterol efflux from peripheral ce...

journal_title：Assay and drug development technologies

authors： Zhang J,Cai S,Peterson BR,Kris-Etherton PM,Heuvel JP

更新日期：2011-04-01 00:00:00

abstract：:In this study, we describe the evaluation of a cell-based protein stability assay using β-galactosidase fragment complementation technology performed in two independent laboratories. The assay is based on the ability of certain ligands to bind to a protein leading to a ligand-protein complex that has a different stabi...

journal_title：Assay and drug development technologies

authors： Auld DS,Davis CA,Jimenez M,Knight S,Orme JP

更新日期：2015-06-01 00:00:00

abstract：:Drug adverse events (AEs) are a major health threat to patients seeking medical treatment and a significant barrier in drug discovery and development. AEs are now required to be submitted during clinical trials and can be extracted from ClinicalTrials.gov ( https://clinicaltrials.gov/ ), a database of clinical studies...

journal_title：Assay and drug development technologies

authors： Federer C,Yoo M,Tan AC

更新日期：2016-12-01 00:00:00

abstract：:The emergence and spread of multidrug-resistant Plasmodium falciparum and recent detection of potential artemisinin-resistant strains in Southeast Asia highlight the importance of developing novel antimalarial therapies. Using a previously generated stable transgenic P. falciparum line with high-level firefly lucifera...

journal_title：Assay and drug development technologies

authors： Che P,Cui L,Kutsch O,Cui L,Li Q

更新日期：2012-02-01 00:00:00

abstract：:The Aurora Biomed-organized annual Ion Channel Retreat occurred in June 2008 and brought together researchers from both academia and industry to share advancements regarding this important field. Topics covered included ion channels as pain targets, ion channels as disease targets, ion channel screening technologies, ...

journal_title：Assay and drug development technologies

authors： Choy N,Davis A,Brugger S,Liang S

更新日期：2008-12-01 00:00:00

abstract：:GPCRs are one of the most popular classes of therapeutic drug targets. It is therefore important to design specific assay formats to readily identify ligands at these receptors. CypHer 5 technology utilizes the general ability of GPCRs to be internalized into the endosomal pathway of a cell in response to agonist liga...

journal_title：Assay and drug development technologies

authors： Adie EJ,Francis MJ,Davies J,Smith L,Marenghi A,Hather C,Hadingham K,Michael NP,Milligan G,Game S

更新日期：2003-04-01 00:00:00

abstract：:NAD synthetase is responsible for the conversion of nicotinic acid adenine dinucleotide to nicotinamide adenine dinucleotide. This reaction provides a biosynthetic route of the coenzyme and, thus, a source of cellular reducing equivalents. Alterations in the oxidative reductive potential of the cell have been implicat...

journal_title：Assay and drug development technologies

authors： Bembenek ME,Kuhn E,Mallender WD,Pullen L,Li P,Parsons T

更新日期：2005-10-01 00:00:00

abstract：:The objective of the present investigation is to enhance the dissolution and flow properties of raloxifene hydrochloride (RXH), a biopharmaceutical classification system class II drug. Melt dispersion of RXH with polyethylene glycol (PEG) 6000 was prepared by the fusion method. The melt dispersion was then adsorbed on...

journal_title：Assay and drug development technologies

authors： Mahajan AN,Surti N,Patel P,Patel A,Shah D,Patel V

更新日期：2020-08-01 00:00:00

abstract：:Despite extensive efforts in tuberculosis (TB) drug research, very few novel inhibitors have been discovered. This issue emphasizes the need for innovative methods to discover new anti-TB drugs. In this study, we established a new high-throughput screen (HTS) platform technology that differs from traditional TB drug s...

journal_title：Assay and drug development technologies

authors： Mai D,Jones J,Rodgers JW,Hartman JL 4th,Kutsch O,Steyn AJ

更新日期：2011-06-01 00:00:00

abstract：:The oncogenic transcription factor signal transducer and activator of transcription 3 (STAT3) is hyperactivated in most cancers and represents a plausible therapeutic target. In the absence of STAT3-selective small-molecule inhibitors, we sought to develop pSTAT3/1 high-content imaging (HCS) assays to screen for selec...

journal_title：Assay and drug development technologies

authors： Johnston PA,Sen M,Hua Y,Camarco D,Shun TY,Lazo JS,Grandis JR

更新日期：2014-01-01 00:00:00

abstract：:Many human diseases result from mutations in specific genes. Once translated, the resulting aberrant proteins may be functionally competent and produced at near-normal levels. However, because of the mutations, the proteins are recognized by the quality control system of the endoplasmic reticulum and are not processed...

journal_title：Assay and drug development technologies

authors： Valenzano KJ,Khanna R,Powe AC,Boyd R,Lee G,Flanagan JJ,Benjamin ER

更新日期：2011-06-01 00:00:00

abstract：:The aim of our work was to establish flow cytometry methods for the characterization of mitochondrial Ca(2+) levels, plasma membrane potential, and superoxide generation and to relate kinetics to that of cytoplasmic Ca(2+) levels during short-term activation of T-lymphocytes. We monitored the change of fluorescence ab...

journal_title：Assay and drug development technologies

authors： Mészáros G,Szalay B,Toldi G,Kaposi A,Vásárhelyi B,Treszl A

更新日期：2012-02-01 00:00:00

abstract：:The central nervous system has been identified as an anatomical reservoir for HIV due the difficulties in delivering therapeutic agents into the brain and this complication results in HIV-associated neurocognitive disorder that persists in infected patients. The brain regions that are potentially exposed to tissue def...

journal_title：Assay and drug development technologies

authors： Mdanda S,Ntshangase S,Singh SD,Naicker T,Kruger HG,Baijnath S,Govender T

更新日期：2019-10-01 00:00:00

abstract：:Recent years have shown a great deal of interest and research into the understanding of the biological and physiological roles of mechanical forces on cellular behavior. Despite these reports, in vitro screening of new molecular entities for lung ailments is still performed in static cell culture models. Failure to in...

journal_title：Assay and drug development technologies

authors： Schmitt S,Hendricks P,Weir J,Somasundaram R,Sittampalam GS,Nirmalanandhan VS

更新日期：2012-04-01 00:00:00

abstract：:Adenosine receptors belong to the superfamily of G protein-coupled receptors and are involved in a variety of physiologic functions. Traditionally, binding assays to detect adenosine 2a (A2a) antagonists and agonists have used filtration methods that are cumbersome to run and not amenable to HTS. We developed scintill...

journal_title：Assay and drug development technologies

authors： Bryant R,McGuinness D,Turek-Etienne T,Guyer D,Yu L,Howells L,Caravano J,Zhai Y,Lachowicz J

更新日期：2004-06-01 00:00:00

abstract：:The diversity and impact of label-free technologies continues to expand in drug discovery. Two classes of label-free instruments, using either an electrical impedance-based or an optical-based biosensor, are now available for investigating the effects of ligands on cellular targets. Studies of GPCR function have been ...

journal_title：Assay and drug development technologies

authors： Peters MF,Vaillancourt F,Heroux M,Valiquette M,Scott CW

更新日期：2010-04-01 00:00:00

abstract：:Embryonic stem (ES) cell technology may serve as a platform for the discovery of drugs to treat diseases such as diabetes. However, because of difficulties in establishing reliable ES cell differentiation methods and in creating cost-effective plating conditions for the high-throughput format, screening for molecules ...

journal_title：Assay and drug development technologies

authors： Chen C,Chai J,Singh L,Kuo CY,Jin L,Feng T,Marzano S,Galeni S,Zhang N,Iacovino M,Qin L,Hara M,Stein R,Bromberg JS,Kyba M,Ku HT

更新日期：2011-08-01 00:00:00

abstract：: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. T...

journal_title：Assay and drug development technologies

authors： Muntean BS,Patil DN,Madoux F,Fossetta J,Scampavia L,Spicer TP,Martemyanov KA

更新日期：2018-04-01 00:00:00