• Proceedings of the PSK Conference
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• 2002.10a
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• pp.181-182
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• 2002

Recentadvancesin '-omics ' technologies enable us to discover more diverse disease- relevant target proteins, which encourages us to find out more target-specific novel lead compounds as new drug candidates. Therefore, high-throughput screening (HTS) becomes an essential tool in this area. Among many HTS tools, in silico HTS is a very fast and cost-effective tool to try to derive a new lead compound for any new targets, especially when the target protein structures are known or readily modeled. (omitted)

• Communications for Statistical Applications and Methods
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• v.27 no.6
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• pp.701-714
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• 2020

Quantitative high throughput screening (qHTS) assays are used to assess toxicity for many chemicals in a short period by collectively analyzing them at several concentrations. Data are routinely analyzed using nonlinear regression models; however, we propose a new method to analyze qHTS data using a nonlinear mixed effects model. qHTS data are generated by repeating the same experiment several times for each chemical; therefor, they can be viewed as if they are repeated measures data and hence analyzed using a nonlinear mixed effects model which accounts for both intra- and inter-individual variabilities. Furthermore, we apply a one-step approach incorporating robust estimation methods to estimate fixed effect parameters and the variance-covariance structure since outliers or influential observations are not uncommon in qHTS data. The toxicity of chemicals from a qHTS assay is classified based on the significance of a parameter related to the efficacy of the chemicals using the proposed method. We evaluate the performance of the proposed method in terms of power and false discovery rate using simulation studies comparing with one existing method. The proposed method is illustrated using a dataset obtained from the National Toxicology Program.

• The Korean Journal of Pesticide Science
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• v.5 no.3
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• pp.41-46
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• 2001

This study was conducted to develop a high throughput system for screening acetolactate synthase(ALS) inhibitors, and to detect basic mother molecules for developing new novel herbicide candidates. The high throughput screening (HTS) method using 96-well plate and microplate reader was developed. This method is 8 times more effective than basic technique in one cycle per person. Futhermore, considering for less than 1/10 volume of materials required for ALS test and enzyme kinetics with 16 times faster speed compared to those of former procedure, this HTS method has more than 100 times higher efficacy than basic system in a consecutive procedure. We discovered 11 new ALS inhibitors such as 2-oxoglutaric acid, aminooxyacetic acid, azelaic acid, citric acid, cyanuric fluoride, itaconic acid, malonic acid, niclosamide, oxalic acid, glyoxylic acid, and suramin from 107 commercial plant-specific inhibitors using this technique. We hope these results might be useful to discover lead compounds for developing new novel herbicide candidate.

• Journal of Life Science
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• v.18 no.9
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• pp.1312-1315
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• 2008

High throughput-drug screening plays a pivotal role for early stage of drug discovery process. In the course of assay development for screening of cell death-inducing agents, a protocol that is simple, time-saving, and high throughput-compatible was designed which was confirmed that the protocol can be worked by a HTS-compatible machine. In 96-well format, PC-3 cancer cells (1${\times}10^{4}$ cells/ml) were cultured for 24 hr. After 24 h-incubation with various medicinal plants extracts, the cells were then stained with DAPI for 30 min. The fluorescence intensity of the stained cells was measured semi-automatically with a multilabel counter. To test whether the present assay system effectively works, we screened about 850 medicinal plant extracts, and selected 1 positive crude extracts that contained cell death-inducing activity. These results suggest that the protocol is highly amenable to HTS implementation for a cell death-inducing agent(s).

• Journal of Marine Bioscience and Biotechnology
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• v.5 no.4
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• pp.33-39
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• 2011

As a rapid and quick bioactive compound evaluation technique, we utilized an automatic system of high throughput screening (HTS) to investigate ${\alpha}$-glucosidase inhibitory efficacy of seaweeds, collected from Jeju Island in Korea. In this study, different extracts with methanol at $20^{\circ}C$ and $70^{\circ}C$ from 23 species of brown seaweeds and 22 species of red seaweeds and 9 species of green seaweeds were subjected to HTS. Of the brown seaweeds tested, Myelophycus simplex (20B3), Ishige sinicola (20B5, 70B5), Colpomenia sinuosa, (20B14, 70B14), Hizikia fusiforme (20B21), Ishige okamurai (70B22) and Ecklonia cava (70B23) showed significantly high ${\alpha}$-glucosidase inhibitory activity with 96.52%, 98.34%, 98.37%, 80.49%, 96.16%, 76.32%, 98.32% and 98.12%. Schizymenia dubyi (20R15), Gelidium amansii (20R16) and Polysiphonia japonica (70R22) amomng the red seaweeds showed remarkable ${\alpha}$-glucosidase inhibitory activity more than 95%. On the other hand, the green seaweeds showed poor ${\alpha}$-glucosidase inhibitory activities (less the10%) at 1 mg/ml.

• Bulletin of the Korean Chemical Society
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• v.32 no.9
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• pp.3229-3232
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• 2011

A FRET-based high-throughput screening system was developed for the discovery of competitive smallmolecule Hsp90 inhibitors. The biarsenical fluorescein derivative FlAsH and dabcyl-conjugated Hsp90 inhibitor GM were employed as the FRET donor and quencher, respectively. The spatial proximity perturbation between FlAsH-labeled Hsp90N and GM-dabcyl upon treatment of a small molecule led to changes in the FRET-induced fluorescence, monitored in a high-throughput fashion.

• Toxicological Research
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• v.25 no.2
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• pp.59-69
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• 2009

Metabolomics which deals with the biological metabolite profile produced in the body and its relation to disease state is a relatively recent research area for drug discovery and biological sciences including toxicology and pharmacology. Metabolomics, based on analytical method and multivariate analysis, has been considered a promising technology because of its advantage over other toxicogenomic and toxicoproteomic approaches. The application of metabolomics includes the development of biomarkers associated with the pathogenesis of various diseases, alternative toxicity tests, high-throughput screening (HTS), and risk assessment, allowing the simultaneous acquisition of multiple biochemical parameters in biological samples. The metabolic profile of urine, in particular, often shows changes in response to exposure to xenobiotics or disease-induced stress, because of the biological system's attempt to maintain homeostasis. In this review, we focus on the most recent advances and applications of metabolomics in toxicological research.

• BMB Reports
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• v.44 no.11
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• pp.705-712
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• 2011

Advances in the fields of proteomics and genomics have necessitated the development of high-throughput screening methods (HTS) for the systematic transformation of large amounts of biological/chemical data into an organized database of knowledge. Microfluidic systems are ideally suited for high-throughput biochemical experimentation since they offer high analytical throughput, consume minute quantities of expensive biological reagents, exhibit superior sensitivity and functionality compared to traditional micro-array techniques and can be integrated within complex experimental work flows. A range of basic biochemical and molecular biological operations have been transferred to chip-based microfluidic formats over the last decade, including gene sequencing, emulsion PCR, immunoassays, electrophoresis, cell-based assays, expression cloning and macromolecule blotting. In this review, we highlight some of the recent advances in the application of microfluidics to biochemistry and molecular biology.

• Proceedings of the Korean Society of Applied Entomolohy Conference
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• 2000.05a
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• pp.77-77
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• 2000

• Journal of Marine Bioscience and Biotechnology
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• v.1 no.3
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• pp.170-177
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• 2006

As a rapid and quick bioactive compound evaluation technique, in this study we utilized a automatic system of High Throughput Screening (HTS) to investigate DPPH radical scavenging efficacy of seaweeds, collected from Jeju Island in Korea. In this study, 6 species of green seaweeds, 18 species of brown seaweeds and 22 species of red seaweeds extracted with methanol at $20^{\circ}C$ and $70^{\circ}C$ were subjected to HTS. Of the green seaweeds tested, Enteromorpha compressa (20G6) of the green seaweeds showed DPPH radical scavenging activity of over 60%. On the other hand, the other green seaweeds showed poor DPPH radical scavenging activities (lees than 40%) at 1 mg/ml. Sargassum siliquastrum (20B17, 70B17), Dictyota dichotoma (70B1), Sargassum coreanum (70B16) and Ecklonia cava (70B26) among the brown seaweeds showed significantly high DPPH radical scavenging activity with 96%, 97%, 92%, 92%, 87%. Polysiphonia japonica (20R24), Schizymenia dubyi (20R17), Gelidium amansii (20R18) and Acrosorium flabellatum (20R23) among the red seaweeds showed remarkable DPPH radical scavenging activity of over 90%.