• Title/Summary/Keyword: Screening system

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Rat Liver $AT_1$ Receptor Binding Analysis for Drug Screening

  • Lee, Sunghou;Lee, Buyean;Hwasup Shin;Jaeyang Kong
    • Biomolecules & Therapeutics
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    • v.3 no.1
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    • pp.21-27
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    • 1995
  • The only compounds with antagonistic activity via AT$_1$receptor, one of two subtypes of angiotensin II (AII) receptor, have been demonstrated to block the vasoconstriction effects of AII and thereby provide therapeutic potential. This initiated the search for compounds with high specific affinity to AT$_1$receptor and their effective screening methods. The radioligand binding assay for the AII receptor is regarded as the primary method for the evaluation of AT$_1$receptor antagonists for their activity. In this paper, we characterized the liver AT$_1$receptor and describe the efficient method of the radioligand binding assay using rat liver as a source of AT$_1$receptor. Equilibrium binding studies with rat adrenal cortex, adrenal medulla, liver and bovine adrenal showed that the specific bindings of [$^3$H] AII were saturable in all tissues and the Scatchard plots of those data were linear, suggesting a single population of binding sites. Hill slopes were very near to the unity in all tissues. Kinetic studies of [$^3$H) AII binding in rat liver homogenates yielded two association rate constants, 4.10$\times$10$^{7}$ M$^{-1}$ min$^{-1}$ and 4.02$\times$10$^{9}$ M$^{-1}$ min$^{-1}$ , with a single dissociation rate constant, 7.07$\times$10$^{-3}$ min-$^{-1}$ , possibly due to the partial dissociation phenomenon. The rank order of inhibition potencies of [$^3$H] AII binding in rat liver was AII>Sarile>Losartan>PD 123177. Rat liver homogenates revealed to have very high density of homogeneous population of the AT$_1$receptor subtype, as the specifically bound [$^3$H] AII was not inhibited by PD 123177, the nonpeptide antagonist of AT$_2$. The results of this study demonstrated that the liver homogenates from rats could be the best receptor preparation for the AT$_1$receptor binding assay and provide an efficient system for the screening of newly synthesized candidate compounds of AT$_1$receptor antagonist.

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Cohort profile: National Investigation of Birth Cohort in Korea study 2008 (NICKs-2008)

  • Kim, Ju Hee;Lee, Jung Eun;Shim, So Min;Ha, Eun Kyo;Yon, Dong Keon;Kim, Ok Hyang;Baek, Ji Hyeon;Koh, Hyun Yong;Chae, Kyu Young;Lee, Seung Won;Han, Man Yong
    • Clinical and Experimental Pediatrics
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    • v.64 no.9
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    • pp.480-488
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    • 2021
  • Background: An adequate large-scale pediatric cohort based on nationwide administrative data is lacking in Korea. Purpose: This study established the National Investigation of Birth Cohort in Korea study 2008 (NICKs-2008) based on data from a nationwide population-based health screening program and data on healthcare utilization for children. Methods: The NICKs-2008 study consisted of the Korean National Health Insurance System (NHIS) and the National Health Screening Program for Infants and Children (NHSPIC) databases comprising children born in 2008 (n=469,248) and 2009 (n=448,459) in the Republic of Korea. The NHIS database contains data on age, sex, residential area, income, healthcare utilization (International Classification of Diseases10 codes, procedure codes, and drug classification codes), and healthcare providers. The NHSPIC consists of 7 screening rounds. These screening sessions comprised physical examination, developmental screening (rounds 2-7), a general health questionnaire, and age-specific anticipatory guidance. Results: During the 10-year follow-up, 2,718 children (0.3%) died, including more boys than girls (hazard ratio, 1.145; P<0.001). A total of 848,048 children participated in at least 1 of the 7 rounds of the NHSPIC, while 96,046 participated in all 7 screening programs. A total of 823 infants (0.1%) weighed less than 1,000 g, 3,177 (0.4%) weighed 1,000-1,499 g, 37,166 (4.4%) weighed 1,500-2,499 g, 773,081 (91.4%) weighed 2,500-4,000 g, and 32,016 (5.1%) weighed over 4,000 g. There were 23,404 premature babies (5.5%) in 2008 compared to 23,368 (5.6%) in 2009. The developmental screening test indicated appropriate development in 95%-98% of children, follow-up requirements for 1%-4% of children, and recommendations for further evaluation for 1% of children. Conclusion: The NICKs-2008, which integrates data from the NHIS and NHSPIC databases, can be used to analyze disease onset prior to hospitalization based on information such as lifestyle, eating habits, and risk factors.

Use of Artificial Intelligence for Reducing Unnecessary Recalls at Screening Mammography: A Simulation Study

  • Yeon Soo Kim;Myoung-jin Jang;Su Hyun Lee;Soo-Yeon Kim;Su Min Ha;Bo Ra Kwon;Woo Kyung Moon;Jung Min Chang
    • Korean Journal of Radiology
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    • v.23 no.12
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    • pp.1241-1250
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    • 2022
  • Objective: To conduct a simulation study to determine whether artificial intelligence (AI)-aided mammography reading can reduce unnecessary recalls while maintaining cancer detection ability in women recalled after mammography screening. Materials and Methods: A retrospective reader study was performed by screening mammographies of 793 women (mean age ± standard deviation, 50 ± 9 years) recalled to obtain supplemental mammographic views regarding screening mammography-detected abnormalities between January 2016 and December 2019 at two screening centers. Initial screening mammography examinations were interpreted by three dedicated breast radiologists sequentially, case by case, with and without AI aid, in a single session. The area under the receiver operating characteristic curve (AUC), sensitivity, specificity, and recall rate for breast cancer diagnosis were obtained and compared between the two reading modes. Results: Fifty-four mammograms with cancer (35 invasive cancers and 19 ductal carcinomas in situ) and 739 mammograms with benign or negative findings were included. The reader-averaged AUC improved after AI aid, from 0.79 (95% confidence interval [CI], 0.74-0.85) to 0.89 (95% CI, 0.85-0.94) (p < 0.001). The reader-averaged specificities before and after AI aid were 41.9% (95% CI, 39.3%-44.5%) and 53.9% (95% CI, 50.9%-56.9%), respectively (p < 0.001). The reader-averaged sensitivity was not statistically different between AI-unaided and AI-aided readings: 89.5% (95% CI, 83.1%-95.9%) vs. 92.6% (95% CI, 86.2%-99.0%) (p = 0.053), although the sensitivities of the least experienced radiologists before and after AI aid were 79.6% (43 of 54 [95% CI, 66.5%-89.4%]) and 90.7% (49 of 54 [95% CI, 79.7%-96.9%]), respectively (p = 0.031). With AI aid, the reader-averaged recall rate decreased by from 60.4% (95% CI, 57.8%-62.9%) to 49.5% (95% CI, 46.5%-52.4%) (p < 0.001). Conclusion: AI-aided reading reduced the number of recalls and improved the diagnostic performance in our simulation using women initially recalled for supplemental mammographic views after mammography screening.

Efficiency Improvement of Environmental Assessment Procedure through Introduction of Screening (스크리닝 도입을 통한 환경평가 절차 효율화 방안)

  • Shin, Kyung-Hee;Cho, Kong-Jang;Yim, Hyo-Sook
    • Journal of Environmental Policy
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    • v.10 no.1
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    • pp.129-150
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    • 2011
  • This paper proposes an improvement to differentiate assessment procedure for projects in consideration of their environmental impact as a means to improve efficiency in environmental impact assessment ("EIA") procedure. The targets of analysis were limited to lower impact projects. The current EA system in Korea has already attempted to introduce separate proceedings for certain projects.Tangible results from these efforts, however, have been limited. Other countries have adopted a "screening" system to determine whether EIA is applicable to a particular project, and if so, what procedure will be used therein. Therefore, this study suggests the screening as the process wherein need for EIA is determined with respect to projects which have undergone Prior Environmental Review System(PERS) and which appear to have comparatively negligible environmental impact. In this case, EIA can be omitted and the developer can then draft a mitigation plan instead. This study found that exempting certain projects deemed as having low environmental impact can considerably shorten the duration required for both environmental assessment and consultation, thereby improving efficiency. Other expected effects from the adoption of this screening include reduction in delays in project execution due to environmental assessments and reduced red tape through the provision of increased autonomy to developers and the approving authorities.

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A Rapid Screening for Aluminum-tolerant and -sensitive in Barley (Hordeum vulgare L.) and Plasma Membrane H+-ATPase Expression (알루미늄 내성과 민감성 보리의 빠른 screening과 원형질막 H+-ATPase의 발현)

  • Kim, Hyun-Sung;Oh, Jung-Min;Ahn, Sung-Ju
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.56 no.1
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    • pp.72-79
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    • 2011
  • Here we report a simple screening system using hematoxylin staining (HS) of the root apex. It allowed rapid classification into different aluminum (Al) tolerance from 65 cultivars within one week. Using this system, we selected the most Al-tolerant (Jayae-2) and-sensitive (Pum-2) barley (Hordeum vulgare L.) The results show that the different responses in Al-induced growth inhibition, Al accumulation and expression of plasma membrane (PM) $H^+$-ATPase in root apices of selected two cultivars. It showed strongly Al-induced growth inhibition in a dosedependant manner only in Pum-2 but not in Jayae-2. Aluminum accumulation in root apices (10 mm) was significantly higher in Pum-2 only. The $H^+$-ATPase expression of PM vesicles by western blotting was decreased in Pum-2 but not in Jayae-2 treated with $20{\mu}M$ Al for 24 h. These finding indicate to screen from our system is rapid and reliable and to sustain the expression of PM $H^+$-ATPase at translational level is an important role in root growth as affected by Al.

Hazard Evaluation of Gas Processes Using a Multi-distinction Equipment Screening Algorithm (다중판별 장치 스크리닝 기법을 이용한 가스공정의 위험성 평가)

  • Yoon En Sup;Park Jeong Su;Ahn Sung Joon;Han Kyounghoon;Yoon Jong Phil;Kim Ku Hwoi;Shin Dongil
    • Journal of the Korean Institute of Gas
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    • v.7 no.1 s.18
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    • pp.1-9
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    • 2003
  • A Multi-distinction Equipment Screening Algorithm (MESA) is proposed. It selectively integrates Dow's F&EI as its process hazard index technique and ESA (Equipment Screening Algorithm) as qualitative hazard classification technique, and retrieves a detailed list of hazardous equipments with the total hazard indices of those equipments. The inherent expert system, which includes the accident scenarios of the equipments and processes and experts' views of them, narrows further down the list of hazardous equipments and recommends only the most notable candidates. Through the case study of distinguishing the hazardous ranking of the equipments of the LPG underground storage process, using the expert system or not, the applicability of MESA has been validated. Taking the characteristics of the process equipments with hazardous ranking in the point of process intrinsic safety, this proposed algorithm would contribute to providing engineers or managers with information on constructing safely devices and mitigation devices and on scheduling emergency response planning.

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Quality Design Support System based on Data Mining Approach (데이터 마이닝 기반의 품질설계지원시스템)

  • 지원철
    • Journal of the Korean Operations Research and Management Science Society
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    • v.28 no.3
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    • pp.31-47
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    • 2003
  • Quality design in practice highly depends on human designer's intuition and past experiences due to lack of formal knowledge about the relationship among 10 variables. This paper represents an data mining approach for developing quality design support system that integrates Case Based Reasoning (CBR) and Artificial Neural Networks (ANN) to effectively support all the steps in quality design process. CBR stores design cases in a systematic way and retrieve them quickly and accurately. ANN predicts the resulting quality attributes of design alternatives that are generated from CBR's adaptation process. When the predicted attributes fail to meet the target values, quality design simulation starts to further adapt the alternatives to the customer's new orders. To implement the quality design simulation, this paper suggests (1) the data screening method based on ξ-$\delta$ Ball to obtain the robust ANN models from the large production data bases, (2) the procedure of quality design simulation using ANN and (3) model management system that helps users find the appropriate one from the ANN model base. The integration of CBR and ANN provides quality design engineers the way that produces consistent and reliable design solutions in the remarkably reduced time.

Cytotoxicity of a Novel Biphenolic Compound, Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane against Human Tumor Cells In vitro

  • Choi, Sang-Un;Kim, Kwang-Hee;Kim, Nam-Young;Choi, Eun-Jung;Lee, Chong-Ock;Son, Kwang-Hee;Kim, Sung-Uk;Bok, Song-Hae;Kim, Young-Kook
    • Archives of Pharmacal Research
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    • v.19 no.4
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    • pp.286-291
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    • 1996
  • Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$, bibenzyl, $2,2^I-dimethylbibenzyl$, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.

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Primary Cultured Brain Cells as Screening Methods for Natural Products Acting on Glutamatergic Neurons (일차배양 뇌세포를 이용한 글루타메이트성 신경에 작용하는 천연물의 검색방법)

  • 박미정;김소라;문애리;김승희;김영중
    • YAKHAK HOEJI
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    • v.39 no.4
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    • pp.444-449
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    • 1995
  • Primary cultures of rat cortical and chicken embryonic brain cells were employed to establish a reliable screening method for natural products blocldng or enhancing glutamate-induced neurotoxicity. Exposure of primary cultured rat cortical cells or chicken embryonic brain cells to high dose of glutamate resulted in the fragmentation of neutites and consequent neuronal death. The level of cytoplasmic lactate dehydrogenase(LDH), indicator for cell survival in cultures, was significantly reduced at exposure to glutamate. For the practical application of the methods, series of concentrations of plants extracts and positive control were applied prior to the glutamate insult on primary cultures of rat cortical and chicken embryonic, brain cells. Relative LDH level in cells was measured for the estimation of the effect of the test materials on the glutamatergic neurons. The validity of the present screening method for natural products acting on glutamatergic neurons was examined with dextromethorphan, a known glutamatergic antagonist. The treatment of 100 $\mu{M}$ dextromethorphan prevented the reduction of LDH in rat cortical and chicken embryonic brain cells caused by glutamate insult keeping 60% and 90% of LDH level in normal control, respectively. Above results indicate that primary cultures of rat cortical and chicken embryonic brain cells could be proper systems for the screening of potential natural agents acting on glutamatergic, neurons. Between the two types of cultures, primary culture of chicken embryonic brain cells seemed to be a better system for the primary screening, since it is technically easier and economical compared to that of rat cortical cells.

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Development of High Throughput Screening Techniques Using Food-borne Library against Anti-asthma Agents (식품소재 라이브러리를 이용한 천식 완화용 물질의 초고속스크리닝 기법 개발)

  • Heo Jin-Chul;Park Ja-Young;Kwon Taeg Kyu;Chung Shin Kyo;Kim Sung-Uk;Lee Sang-Han
    • Food Science and Preservation
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    • v.12 no.3
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    • pp.267-274
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    • 2005
  • Oxidant stress is a well-known pivotal parameter for the degenerative immune diseases including asthma, atopic dermatitis, and rhinitis. In order to screen for anti-asthma agents effectively, we first established the infrastructure of high throughput screening(HTS) for anti-oxidant agents from agricultural products and/or oriental medicine library extracted with water, methanol, dimethyl sulfoxide, ethyl acetate and juice, Using the screening system, we found that Chaenomelis langenariae, Rhus javanica L., Camellia sinensis, Helianthus annuus and Angelica utilis Makino had strong anti-oxidant activity. Moreover, Helianthus annuus, Rehmannia glutinosa Libo and Angelica utilis Makino have protection activities by treatment of an oxidant hydrogen peroxide. Together, these results suggest that screened agents could be potential agents against asthma, although the in vivo studies should be clearly tested.