• Title/Summary/Keyword: dual targets

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Comparative Reverse Screening Approach to Identify Potential Anti-neoplastic Targets of Saffron Functional Components and Binding Mode

  • Bhattacharjee, Biplab;Vijayasarathy, Sandhya;Karunakar, Prashantha;Chatterjee, Jhinuk
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.11
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    • pp.5605-5611
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    • 2012
  • Background: In the last two decades, pioneering research on anti-tumour activity of saffron has shed light on the role of crocetin, picrocrocin and safranal, as broad spectrum anti-neoplastic agents. However, the exact mechanisms have yet to be elucidated. Identification and characterization of the targets of bioactive constituents will play an imperative role in demystifying the complex anti-neoplastic machinery. Methods: In the quest of potential target identification, a dual virtual screening approach utilizing two inverse screening systems, one predicated on idTarget and the other on PharmMapper was here employed. A set of target proteins associated with multiple forms of cancer and ranked by Fit Score and Binding energy were obtained from the two independent inverse screening platforms. The validity of the results was checked by meticulously analyzing the post-docking binding pose of the picrocrocin with Hsp90 alpha in AutoDock. Results: The docking pose reveals that electrostatic and hydrogen bonds play the key role in inter-molecular interactions in ligand binding. Picrocrocin binds to the Hsp90 alpha with a definite orientation appropriate for nucleophilic attacks by several electrical residues inside the Hsp90-alpha ATPase catalytic site. Conclusion: This study reveals functional information about the anti-tumor mechanism of saffron bioactive constituents. Also, a tractable set of anti-neoplastic targets for saffron has been generated in this study which can be further authenticated by in vivo and in vitro experiments.

Development of Unfolding Radial Velocity Algorithm for Dual PRF Mode of Yong-In Testbed(YIT) Radar (용인테스트베드레이다를 이용한 Dual PRF 모드의 시선속도 접힘 풀기 알고리즘 개발)

  • Kim, Hye-Ri;Suk, Mi-Kyung;Nam, Kyung-Yeub;Ko, Jeong-Seok
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.27 no.6
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    • pp.521-530
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    • 2016
  • Weather radar is observation equipment that transmits electromagnetic waves and receives backscattered signals from the targets. The weather radar systems of the Korea Meteorological Administration have a doppler mode that can extract the target's radial velocity. However, the radial velocity over the maximum unambiguous velocity(${\nu}_m$) for which is in a trade-off relationship with the maximum unambiguous range is folded. Therefore, a dual PRF mode of which transmits and receives signals using two different PRFs(high and low) must be used to extend the vm while maintaining the maximum unambiguous range. Using a dual PRF mode, vm can be extended to the amount of lowest common denominator of two observed vm from high and low PRF. For this extension, we have developed a velocity unfolding algorithm of which uses several criteria for classification considering observed velocity differences between high and low PRF and their error boundary. Then, correction factors are calculated for each class and are applied to unfold radial velocity. The developed algorithm was applied to the Yong-In Testbed(YIT) radar and the generated better performance of radial velocity extraction than those of the previous system.

The study on target recognition method to process real-time in W-band mmWave small radar (밀리미터파대역(W-대역)공대지 레이다의 이중편파 채널을 활용한 지상 표적 식별 기법에 관한 연구)

  • Park, Sungho;Kong, Young-Joo;Ryu, Seong-Hyun;Yoon, Jong-Suk
    • The Journal of the Institute of Internet, Broadcasting and Communication
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    • v.18 no.3
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    • pp.61-69
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    • 2018
  • In this paper, we propose a method for recognizing ground target using dual polarization channels in millimeter waveband air-to-surface radar. First, the Push-Broom target detection method is described and the received signal is modeled considering flight-path scenario of air-to-surface radar. The scattering centers were extracted using the RELAX algorithm, which is a time domain spectral estimation technique, and the feature vector of the target was generated. Based on this, a DB for 4 targets is constructed. As a result of the proposed method, it is confirmed that the target classification rates is improved by more than 15% than the single channel using the data of the dual polarization channel.

Dual Drug-Loaded Liposomes for Synergistic Efficacy in MCF-7 Breast Cancer Cells and Cancer Stem Cells

  • Park, Hee-Bin;Kim, Yun-Ji;Lee, Seong-Min;Park, James S.;Kim, Keun-Sik
    • Biomedical Science Letters
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    • v.25 no.2
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    • pp.159-169
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    • 2019
  • Breast cancer stem cells (BCSCs) in breast cancer cells have self-renewal ability and differentiation potential. They are also resistant to drugs after chemotherapy. To overcome this resistance, we designed negatively charged 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG)-based liposomes for drug delivery. These liposomes have enhanced the therapeutic effects of a range of antitumor therapies by increasing the cellular uptake and improving drug delivery to targets sites. In this study, we investigated whether DMPG-POPC liposomes, including the neutral lipid 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholin (POPC), can specifically bind to MCF-7 breast cancer cells and increase cellular uptake compared with that by CHOL-POPC liposomes. We also estimated the cytotoxicity of DMPG-POPC liposomes encapsulated with both metformin (Met) and sodium salicylate (Sod) against breast cancer cells and BCSCs compared with that of the free drugs. Our results demonstrated that these dual drug-encapsulated liposomes significantly enhanced the cytotoxic and anti-colony formation abilities compared with individual drug-encapsulated liposomes or free drugs in BCSCs. Overall, our results suggest that DMPG-POPC liposomes containing two drugs (Met + Sod) show promise for synergistic anti-cancer therapy of breast cancer by increasing drug delivery efficiency into breast cancer cells and BCSCs.

Detection of AGN outflows in micro-arcsec scales

  • Oh, Junghwan;Trippe, Sascha;Krichbaum, Thomas;Sohn, Bong Won;Bremer, Michael
    • The Bulletin of The Korean Astronomical Society
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    • v.38 no.2
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    • pp.43.1-43.1
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    • 2013
  • We report the preliminary results of our GMVA(Global mm VLBI Array) observation at the frequency of 86 GHz. Observation were made in the dual polarization mode (LCP and RCP), to produce the polarimetric maps with the maximum angular resolution which the array is capable of. We aim to link the source-integrated AGN polarization properties with the polarized spatial source structure, by mapping the polarized "fine structure" of the target AGN. We selected 2 targets, 0954+658 and 0716+714, which (1) have been observed multiple times by the PdBI polarimetric monitoring program; (2) have sufficient integrated fluxes ($S_{90GHz}$ > 1 Jy) ; (3) are close enough to resolve the source structure < 1 pc with given angular resolution ; and (4) are located at high northern declination for good UV coverages. As preliminary results, we present LL and RR polarized images of each target with the maximum angular resolution of ${\sim}60{\mu}as$. Extended structures, probably the jet outflows, are discovered in both sources.

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Characterization of Cu-Ni alloy thin films deposited by magnetron co-sputtering as a function of target configurations (마그네트론 코-스퍼터링에 의한 구리-니켈 합금박막 증착시 타겟의 구성방법에 따른 물성 분석)

  • SEO, Soo-Hyung;LEE, Jae-Yup;PARK, Chang-Kyun;PARK, Jin-Seok
    • Proceedings of the KIEE Conference
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    • 2000.07c
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    • pp.1485-1487
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    • 2000
  • A variety of target configurations in sputtering process have been proposed to deposit various structures of thin film alloys and compound films. In this study, we presented the comparative experimental results regarding to the characterization of properties of Cu-Ni thin films deposited by using a magnetron co-sputtering method, as a function of target configurations; one is using a single target with varying the area of Ni chips attached on the Cu target and another is using a dual-type target with two targets of Ni and Cu separated each other. Structural(d-spacing, crystal orientation, crystallite size, cross-sectional morphology) and electrical(resistivity) properties of deposited films are characterized and compared as a function of target configurations as well as deposition conditions.

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Improvement of LECEEP Protocol through Dual Chain Configuration in WSN Environment(A-LECEEP, Advanced LEACH based Chaining Energy Efficient Protocol) (WSN 환경에서 이중체인 구성을 통한 LECEEP 프로토콜 개선(A-LECEEP))

  • Kim, Chanhyuk;Kwon, Taewook
    • Journal of Korea Multimedia Society
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    • v.24 no.8
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    • pp.1068-1075
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    • 2021
  • Wireless sensor network (WSN) can be usefully used in battlefields requiring rapid installation and operation by enabling surveillance and reconnaissance using small sensors in areas where any existing network infrastructure is not formed. As WSN uses battery, energy efficiency acts as a very important issue in network survivability. Layer-based routing protocols have been studied a lot in the aspect of energy efficiency. Many research selected LEACH and PEGASIS protocols as their comparison targets. This study examines the two protocols and LECEEP, a protocol designed by combining their advantages, and proposes a new protocol, A-LECEEP, which is more energy efficient than the others. The proposed protocol can increase energy efficiency compared to the existing ones by eliminating unnecessary transmissions with multiple chains configuration.

Crosstalk between the Producers and Immune Targets of IL-9

  • Van Anh Do-Thi;Jie-Oh Lee;Hayyoung Lee;Young Sang Kim
    • IMMUNE NETWORK
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    • v.20 no.6
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    • pp.45.1-45.16
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    • 2020
  • IL-9 has been reported to play dual roles in the pathogenesis of autoimmune disorders and cancers. The collaboration of IL-9 with microenvironmental factors including the broader cytokine milieu and other cellular components may provide important keys to explain its conflicting effects in chronic conditions. In this review, we summarize recent findings on the cellular sources of, and immunological responders to IL-9, in order to interpret the role of IL-9 in the regulation of immune responses. This knowledge will provide new perspectives to improve clinical benefits and limit adverse effects of IL-9 when treating pathologic conditions.

Ultrasound Targeted Microbubble Destruction for Novel Dual Targeting of HSP72 and HSC70 in Prostate Cancer

  • Wang, Hang-Hui;Song, Yi-Xin;Bai, Min;Jin, Li-Fang;Gu, Ji-Ying;Su, Yi-Jin;Liu, Long;Jia, Chao;Du, Lian-Fang
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.3
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    • pp.1285-1290
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    • 2014
  • The aim was to determine whether ultrasound targeted microbubble destruction (UTMD) promotes dual targeting of HSP72 and HSC70 for therapy of castration-resistant prostate cancer (CRPC), to improve the specific and efficient delivery of siRNA, to induce tumor cell specific apoptosis, and to find new therapeutic targets specific of CRPC.VCaP cells were transfected with siRNA oligonucleotides. HSP70, HSP90 and cleaved caspase-3 expression were determined by real-time quantitative polymerase chain reaction and Western blotting. Apoptosis and transfection efficiency were assessed by flow cytometry. Cell viability assays were used to evaluate safety. We found HSP72, HSC70 and HSP90 expression to be absent or weak in normal prostate epithelial cells (RWPE-1), but uniformly strong in prostate cancerous cells (VCaP). UTMD combined with dual targeting of HSP72 and HSC70 siRNA improve the efficiency of transfection, cell uptake of siRNA, downregulation of HSP70 and HSP90 expression in VCaP cells at the mRNA and protein level, and induction of extensive tumor-specific apoptosis. Cell counting kit-8 assays showed decreased cellular viability in the HSP72/HSC70-siRNA silenced group. These results suggest that the combination of UTMD with dual targeting HSP70 therapy for PCa may be most efficacious, providng a novel, reliable, non-invasive, safe targeted approach to improve the specific and efficient delivery of siRNA, and achieve maximal effects.

MicroRNA-200a Targets Cannabinoid Receptor 1 and Serotonin Transporter to Increase Visceral Hyperalgesia in Diarrhea-predominant Irritable Bowel Syndrome Rats

  • Hou, Qiuke;Huang, Yongquan;Zhang, Changrong;Zhu, Shuilian;Li, Peiwu;Chen, Xinlin;Hou, Zhengkun;Liu, Fengbin
    • Journal of Neurogastroenterology and Motility
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    • v.24 no.4
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    • pp.656-668
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    • 2018
  • Background/Aims MicroRNAs (miRNAs) were reported to be responsible for intestinal permeability in diarrhea-predominant irritable bowel syndrome (IBS-D) rats in our previous study. However, whether and how miRNAs regulate visceral hypersensitivity in IBS-D remains largely unknown. Methods We established the IBS-D rat model and evaluated it using the nociceptive visceral hypersensitivity test, myeloperoxidase activity assay, restraint stress-induced defecation, and electromyographic (EMG) activity. The distal colon was subjected to miRNA microarray analysis followed by isolation and culture of colonic epithelial cells (CECs). Bioinformatic analysis and further experiments, including dual luciferase assays, quantitative real-time polymerase chain reaction, western blot, and enzyme-linked immunosorbent assay, were used to detect the expression of miRNAs and how it regulates visceral hypersensitivity in IBS-D rats. Results The IBS-D rat model was successfully established. A total of 24 miRNAs were differentially expressed in the distal colon of IBS-D rats; 9 were upregulated and 15 were downregulated. Among them, the most significant upregulation was miR-200a, accompanied by downregulation of cannabinoid receptor 1 (CNR1) and serotonin transporter (SERT). MiR-200a mimic markedly inhibited the expression of CNR1/SERT. Bioinformatic analysis and luciferase assay confirmed that CNR1/SERT are direct targets of miR-200a. Rescue experiments that overexpressed CNR1/SERT significantly abolished the inhibitory effect of miR-200a on the IBS-D rats CECs. Conclusions This study suggests that miR-200a could induce visceral hyperalgesia by targeting the downregulation of CNR1 and SERT, aggravating or leading to the development and progression of IBS-D. MiR-200a may be a regulator of visceral hypersensitivity, which provides potential targets for the treatment of IBS-D.