• Title/Summary/Keyword: RAR

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A Potential Target of Tanshinone IIA for Acute Promyelocytic Leukemia Revealed by Inverse Docking and Drug Repurposing

  • Chen, Shao-Jun
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.10
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    • pp.4301-4305
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    • 2014
  • Tanshinone IIA is a pharmacologically active ingredient extracted from Danshen, a Chinese traditional medicine. Its molecular mechanisms are still unclear. The present study utilized computational approaches to uncover the potential targets of this compound. In this research, PharmMapper server was used as the inverse docking tool andnd the results were verified by Autodock vina in PyRx 0.8, and by DRAR-CPI, a server for drug repositioning via the chemical-protein interactome. Results showed that the retinoic acid receptor alpha ($RAR{\alpha}$), a target protein in acute promyelocytic leukemia (APL), was in the top rank, with a pharmacophore model matching well the molecular features of Tanshinone IIA. Moreover, molecular docking and drug repurposing results showed that the complex was also matched in terms of structure and chemical-protein interactions. These results indicated that $RAR{\alpha}$ may be a potential target of Tanshinone IIA for APL. The study can provide useful information for further biological and biochemical research on natural compounds.

Parameter Selection Procedure of Parabolic Reflector Antenna for the Optimum Synthetic Aperture Radar Performances

  • Yoon, Seong Sik;Lee, Jae Wook;Lee, Taek Kyung;Yi, Dong Woo
    • Journal of electromagnetic engineering and science
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    • v.13 no.4
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    • pp.251-258
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    • 2013
  • A procedure for antenna parameter selections is proposed that considers the relationships between synthetic aperture radar performance and the antenna parameters of a parabola-type reflector antenna with a central flat dish. The effects of a central dish designed for weight reduction on the antenna beam pattern are also quantitatively analyzed using commercially available software based on the physical optics algorithm. The results of the theoretical analysis and simulation predict that a larger size of the central dish results in an increase in the sidelobe level, which is the reason for the increase in two important ambiguities, such as range ambiguity ratio (RAR) and azimuth ambiguity ratio (AAR). The dependence of RAR and AAR on Pulse repetition frequency is also analyzed and discussed.

Studies on Biochemical Mechanism of DNA Alkylating Agents Tethered to Ligands for Retinoic acid Receptor

  • Yun, Byoung-Gu;Pyun, Sung-Jae;Ji, Sang-Mi;Ham, Won-Hoon;Lee, Young-Joo;Park, Hyun-Ju
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.176.2-176.2
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    • 2003
  • Transcription factors (TF) can bind tightly to specific DNA lesions formed by some anticancer agents. The formation these TF:(drug-modified DNA) complex may disrupt expression of genes critical for cell survival, and it was proved to be one of biochemical mechanisms of anticancer activity. Based on this model, we have designed programmable DNA Alkylating agents that can also attract TF, especially nuclear receptors. As a model compound, we designed drug molecules, RA-mustard and Am580-mustard, that enable to bind both retinoic acid receptor (RAR) and DNA by using molecular modeling techniques, and synthesized them by connecting chlorambucil and ligand for RAR with a linker unit. (omitted)

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Combined Effects Methylation of FHIT, RASSF1A and RARβ Genes on Non-Small Cell Lung Cancer in the Chinese Population

  • Li, Wen;Deng, Jing;Tang, Jian-Xin
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.13
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    • pp.5233-5237
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    • 2014
  • Epigenetic modifications of tumour suppressor genes are involved in all kinds of human cancer. Aberrant promoter methylation is also considered to play an essential role in development of lung cancer, but the pathogenesis remains unclear.We collected the data of 112 subjects, including 56 diagnosed patients with lung cancer and 56 controls without cancer. Methylation of the FHIT, RASSF1A and RAR-${\beta}$ genes in DNA from all samples and the corresponding gene methylation status were assessed using the methylation-specific polymerase chain reaction (PCR, MSP). The results showed that the total frequency of separate gene methylation was significantly higher in lung cancer compared with controls (33.9-85.7 vs 0 %) (p<0.01).Similar outcomes were obtained from the aberrant methylation of combinations of any two or three genes (p<0.01). There was a tendency that the frequency of combinations of any two or three genes was higher in stage I+II than that in stage III+IV with lung cancer. However, no significant difference was found across various clinical stages and clinic pathological gradings of lung cancer (p>0.05).These observations suggest that there is a significant association of promoter methylation of individual genes with lung cancer risk, and that aberrant methylation of combination of any two or three genes may be associated with clinical stage in lung cancer patients and involved in the initiation of lung cancer tumorigenesis. Methylation of FHIT, RASSF1A and $RAR{\beta}$ genes may be related to progression of lung oncogenesis.

A Novel All-trans Retinoid Acid Derivative Induces Apoptosis in MDA-MB-231 Breast Cancer Cells

  • Wang, Bei;Yan, Yun-Wen;Zhou, Qing;Gui, Shu-Yu;Chen, Fei-Hu;Wang, Yuan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.24
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    • pp.10819-10824
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    • 2015
  • Aims: To explore the effect and probable mechanism of a synthetic retinoid 4-amino-2-tri-fluoromethylphenyl ester (ATPR) on apoptosis of MDA-MB-231 breast cancer cells. Materials and Methods: MTT assays were performed to measure the proliferation of MDA-MB-231 cells treated with different concentrations of all-trans retinoic acid (ATRA) and ATPR. Morphologic changes were observed by microscopy. The apoptosis rates and cell cycling of MDA-MB-231 cells treated with ATRA or ATPR were assessed using flow cytometry analysis. Expression of retinoic acid receptor and phosphorylation of ERK, JNK, p38 proteins were detected by Western blotting. Results: Treatment of the cells with the addition of $15{\mu}mol/L$ ATPR for 48 h clearly demonstrated reduced cell numbers and deformed cells, whereas no changes in the number and morphology were observed after treatment with ATRA. The apoptosis rate was 33.2% after breast cancer MDA-MB-231 cells were treated by ATPR ($15{\mu}mol/L$) whereas ATRA ($15{\mu}mol/L$) had no apoptotic effect. ATPR inhibited the phosphorylation of ERK, JNK, and p38 while ATRA had no significant effect. ATPR inhibited the expression of BiP and increased the expression of Chop at the protein level compared with control groups, ATRA and ATPR both decreased the protein expression of $RXR{\alpha}$, ATPR reduced the protein expression of $RAR{\beta}$ and $RXR{\beta}$ while ATRA did not decrease $RAR{\beta}$ or $RXR{\beta}$. Conclusions: ATPR could induce apoptosis of breast cancer MDA-MB-231 cells, possible mechanisms being binding to $RAR{\beta}/RXR{\beta}$ heterodimers, then activation of ER stress involving the MAPK pathway.

Construction and evaluation of the radar-AWS accumulated rainfall calculation system (레이더-AWS 누적강수량 산출 시스템 구축 및 평가)

  • Ko, Hye-Young;Nam, Kyung-Yeub;Chang, Ki-Ho;Choi, Young-Jean
    • Proceedings of the Korea Water Resources Association Conference
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    • 2011.05a
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    • pp.94-94
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    • 2011
  • 최근에 산악지역에서의 국지성 강우에 의한 사고 발생이 증가하고 있고, 2009년에는 북한의 무단 댐방류로 인해 인명피해가 발생함에 따라서 산악이나 북한 지역과 같은 지역의 모니터링이 필요하게 되었으며, 강수량의 기후학적 분포의 특성과 같은 장기적인 강수량 정보가 필요하게 되었다. 레이더는 넓은 영역에 대해서 시 공간적으로 고해상도의 자료를 제공할 수 있기 때문에 국지 규모의 단시간 강수량 정보를 제공하는데 유용하다. 국립기상연구소(National Institute of Meteorological Research; NIMR)는 기존의 층운형 Z-R 관계식(Z=$200R^{1.6}$, Marshall-Palmer, 1948)을 이용한 레이더 강우강도 산출에서 과소추정 문제를 개선하기 위해 레이더-AWS 강우강도(Radar-AWS Rain rate; RAR) 산출 시스템을 개발하여 현재 운영하고 있다. RAR 산출 알고리즘은 각 레이더에 대해서 레이더 강우강도와 지상 AWS 우량계 자료를 비교하여 실시간으로 Z-R 관계식을 산출하여, 레이더 반사도를 강우강도로 변환하고, 이를 합성하여 한반도 영역에 대해서 강우강도 정보를 제공한다. 2010년에는 RAR 자료와 지상 AWS 우량계 자료를 이용하여 레이더-AWS 누적강수량을 산출하는 시스템을 구축하였으며, 현재 시험운영 중에 있다. 본 연구에서는 레이더-AWS 누적강수량의 정확도를 평가하기 위해서 2009년에 대해 레이더-AWS 누적강수량 자료와 지상 AWS 누적강수량 자료에 대해 RMSE, Bias 등의 통계값을 산출하였으며, 북한 지역에 대한 적용가능성을 분석하기 위해서 레이더 관측 반경 내의 북한 지역의 GTS 지점 자료를 이용하여 사례 분석하였다. 본 연구는 레이더 자료를 이용한 지상 관측 공백지역의 강수량에 대한 모니터링을 통하여 이러한 지역의 사고에 대비할 수 있고, 기후학적인 강수량 정보 제공 및 향후 유역별 레이더 면적강수지도 시험판 개발을 통하여 수문 기상 분야에 적용하여 효과적인 물관리에 기여할 수 있을 것으로 사료된다.

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Economic Evaluation on Geosynthetic Reinforced Abutment for Railways (특정형상의 인공자갈이 혼합된 도상자갈층의 지지성능과 응력전달특성)

  • Kim, Dae Sang
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.12
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    • pp.15-20
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    • 2019
  • This paper evaluated the construction costs of 11 design cases to decrease the horizontal forces applied to the abutment. They include two abutment types, which are to improve backfill materials for a reversed T-shaped abutment and geosynthetic Reinforced Abutment for Railways (RAR). The first type of economic analysis was that the internal friction angles of backfill materials were increased from Φ=35° to Φ=40° and 50° for a reversed T-shaped abutment. In addition, the second type was the cases with the design of geosynthetic RAR. When friction angles of 40° or 50° were applied through the improvement of the backfill material, the decrease in construction cost of the abutment was not large (2.0~3.9%), even though the horizontal forces applied to the abutment had decreased to 18~48%. In the case of applying the RAR, however, a maximum 30% cost reduction was evaluated by the decrease in horizontal force to "0" theoretically. The cost reduction resulted from the decrease in wall thickness, base slab size, and number and material change of pile foundation for the abutment.

Application of the weather radar-based quantitative precipitation estimations for flood runoff simulation in a dam watershed (기상레이더 강수량 추정 값의 댐 유역 홍수 유출모의 적용)

  • Cho, Younghyun;Noh, Joon Woo;Lee, Eul Rae
    • Proceedings of the Korea Water Resources Association Conference
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    • 2019.05a
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    • pp.61-61
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    • 2019
  • 우리나라는 대부분이 산지(약 65%)로 구성되어 있어 강우 시 그 공간적 분포의 변동성이 매우 큰 편이며, 특히 전형적인 산지지형인 댐 유역의 경우 고도 변화 등에 기인한 지형특성 등에 따라 강우의 형태 및 패턴과 이에 따른 유출변화가 큰 복잡한 특성을 갖는다. 이로 인해 단순히 지점강우들을 공간보간(평균)한 면적강우를 홍수 유출모의 등에 활용할 경우 그 신뢰도가 매우 낮은 경우가 많아, 수문모의에 있어 레이더에 기반을 둔 공간 분포형 강우 등의 도입 검토가 요구된다. 한편, 최근 기상청에서는 보다 정확한 레이더 강수량 추정 값의 제공을 위해 "레이더-AWS 강우강도(Radar-AWS Rainrates, RAR)" 산출 기술을 지속적으로 개선하고 있으며, 이는 지상 우량계 대비 상당한 정확도를 보이고 있다. 본 연구에서는 국내 산지지형을 대표하며, 타 댐 유역에 비해 비교적 수문(수위/유량)관측소와 자료가 많은 용담시험유역에 기상레이더 강수량 추정 값(RAR)을 적용해 산지지형 댐 유역에서 강우의 시공간적 변동성과 이에 따른 홍수량의 정확한 분석을 통해 홍수 시 댐 유입량의 정확한 산정 등에 활용할 목적으로 홍수 유출모의를 수행하고자 한다. 모의에는 최근 5년(2014~2018년)동안 발생한 비교적 독립적인 1~2개(연도별)의 홍수사상을 적용하였으며, 모형은 분포형 강우를 적용할 수 있는 비교적 간단한 모형인 HEC-HMS를 활용하였다. HEC-HMS는 주로 집중형 수문모형(Lumped Hydrologic Model)으로 분류되어 레이더 강우와 같은 분포형 자료의 입력을 주로 적용치는 않고 있지만, HEC-GeoHMS와 ModClark 방법을 활용하면 격자단위의 분포형 강우를 적용할 수 있는 형태의 모델 구축이 가능하다. 모의 결과는 기존 유역평균 강우를 적용한 방법과 비교를 통해 그 개선점을 검토하고자 하며, 이를 통하여 산지지역 댐 유역의 홍수특성을 보다 더 정확하게 분석해보고자 한다. 한편, ModClark을 적용한 홍수 유출모의는 단순히 소유역별 도달시간의 격자별 비율을 고려한 홍수추적으로 그 해석상의 한계가 있어, 최근 개발된 하이브리드 수문모형(Hybrid Hydrologic Model, Distributed-Clark) 등도 동일유역에 대해 도입 적용할 계획에 있다.

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