• Title/Summary/Keyword: target molecule

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Detection of Molecules using the Nanoparticle Arrays (나노입자 배열을 이용한 분자 검출)

  • Ha, Dong-Han;Kim, Sang-Hun;Yun, Yong-Ju;Park, Hyung-Ju;Yun, Wan-Soo
    • Proceedings of the KSME Conference
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    • pp.1617-1622
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    • 2008
  • We report a new molecular detection process which measures the changes in the plasmon resonance peaks of periodic Au nanoparticle arrays fabricated using the electron beam lithography. As the Au nanoparticle arrays are modified by the chemical reaction in solutions having various concentrations of a target molecule, both the position and intensity of the plasmon peak change in proportion to the concentration of the target molecule. We expect that the process developed in this work can be employed for fine tuning of the plasmon peak wavelength and also for the optical detection of various kinds of molecules. Moreover, this method may improve the measurement accuracy compared with existing approaches that use only one change (peak wavelength or peak intensity) as a readout value for the molecular detection.

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새로운 퀴놀론 항균제의 합성

  • 강석구
    • Proceedings of the Korean Society of Applied Pharmacology
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    • pp.227-227
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    • 1994
  • 퀴놀론계 항균제란 퀴놀린 이나 나프티리딘 핵을 갖고 있는 화합물로써 항균효과를 나타내는 물질을 의미한다. 이러한 퀴놀론계 항균제의 구조적 특성에 따라 항균활성의 영향은 ASAR에 의하여 이미 구조적 제한성을 가지고 있다고 보고 되어있다. 본 연구에서는 Drug-Enzyme inleraetion domain을 변화시킴으로서 보다 강력한 항균제를 찾아낼수 있을 것으로 판단하고, 기존 항균제가 C-7에 piperazine이 있으므로 piperazine의 chemical isoster 또는 bioisoster의 개념하에서 C-7에 도입한 아민류를 분자설계하고 합성하여 새로운 퀴놀론계 항균제를 만들어 내고자 하였으며 target molecule은 다음 그림과 같다.

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Synthesis of a Conformationally-rigid Etorphine Analogous

  • Kim, Keun-Jae;Hahn, Soon-Jong;Lyu, Hark-Soo
    • Bulletin of the Korean Chemical Society
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    • v.7 no.3
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    • pp.166-169
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    • 1986
  • In order to synthesize conformationally rigid etorphine analogues having potentially interesting pharmacological activities, synthesis of compound 3 by the reaction of compound 4 and compound 5 via intramolecular Diels-Alder reaction has been attempted. However, the reaction did not go well and the compound 3 would not be isolated. Therefore, intermolecular Diels-Alder reaction using dimethyl acetylene dicarboxylate was attempted. As shown in scheme 2, Diels-Alder adduct 9 was converted into the target molecule 14 containing the new [2.2.2] bicyclo octane ring in good yields.

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Expression and Function of GSTA1 in Lung Cancer Cells

  • Pan, Xue-Diao;Yang, Zhou-Ping;Tang, Qi-Ling;Peng, Tong;Zhang, Zheng-Bing;Zhou, Si-Gui;Wang, Gui-Xiang;He, Bing;Zang, Lin-Quan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.20
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    • pp.8631-8635
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    • 2014
  • Glutathione S-transferase A1 (GSTA1) appears to be primarily involved in detoxification processes, but possible roles in lung cancer remain unclear. The objective of this study was to investigate the expression and function of GSTA1 in lung cancer cells. Real-time PCR and Western blotting were performed to assess expression in cancer cell lines and the normal lung cells, then verify the A549 cells line with stable overexpression. Localization of GSTA1 proteins was assessed by cytoimmunofluorescence. Three double-strand DNA oligoRNAs (SiRNAs) were synthesized prior to being transfected into A549 cells with Lipofectamine 2000, and then the most efficient SiRNA was selected. Expression of the GSTA1 gene in the transfected cells was determined by real-time PCR and Western blotting. The viability of the transfected cells were assessed by MTT. Results showed that the mRNA and protein expression of A549 cancer cells was higher than in MRC-5 normal cells. Cytoimmunofluorescence demonstrated GSTA1 localization in the cell cytoplasm and/or membranes. Transfection into A549 cells demonstrated that down-regulated expression could inhibit cell viability. Our data indicated that GSTA1 expression may be a target molecule in early diagnosis and treatment of lung cancer.

Cyclooxygenase-2 Expression in Urinary Bladder Transitional Cell Carcinoma and its Association with Clinicopathological Characteristics

  • Tabriz, Hedieh Moradi;Olfati, Golrokh;Ahmadi, Seyed Ali;Yusefnia, Sudabeh
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.8
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    • pp.4539-4543
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    • 2013
  • Background: Transitional cell carcinoma (TCC) is the most predominant type of urinary bladder tumor. As cyclooxygenase (COX)-2 is recently introduced as an attractive target molecule in bladder TCC, we evaluated the immunohistochemical expression of this marker and its association with several clinicopathological characteristics. Materials and Methods: This cross-sectional study was performed in the Pathology department of Sina Hospital in Tehran, Iran during 2006-2011. Ninety-two paraffin embedded blocks were selected from patients with urinary bladder TCC who underwent cystectomy or transurethral resection (TUR). Then, we assessed COX-2 expression by immunohistochemical staining using antibody against COX-2. Staining in more than 5% of tumor cells was considered as positive expression. Results: COX-2 was expressed in 50 % of our patients. This marker was markedly expressed in high grade bladder TCC (62.1%) versus other grades and there was statistically a significant difference in COX-2 expression between various grades (p=0.008). In addition, patients' age, lymphatic and perineurial invasion were associated with the expression of COX-2 (p=0.001, 0.015 and 0.039, respectively). However, other parameters such as stage, tumor size, venous invasion and lymph node metastasis did not show any significant relationship with this marker (all, p>0.05). Conclusions: COX-2 was expressed in urinary bladder TCC especially in high grade forms, advocating its probable role in the differentiation of this tumor. Accordingly, COX-2 could be a valuable biological target molecule in the evaluation and treatment of patients with bladder TCC.

Multiple Functional Effects of Korea Ginseng on Vascular Endothelial Cells

  • Kim, Young-Myeong;Lee, Young-Chul
    • Proceedings of the Ginseng society Conference
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    • pp.13-17
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    • 2006
  • 다양한 연구에 따르면, 고려인삼은 허약한 체질, 숙취, 폐경과 월경불순, 초기 당뇨병, 영양실조, 빈혈 및 단백질 부족, 간기능 악화, 각종 독성물질에 기인한 중독, 피로, 추위, 스트레스, 산후조리, 체력쇠퇴 등에 효능이 있음이 알려져 있다. 특히 고려인삼은 혈관 기능을 효과적으로 조절함으로 고혈압, 뇌졸중, 심근경색, 동맥경화, 관절염, 당뇨, 비만 등의 질환을 효과적으로 치료하거나 예방할 수 있는 효능이 있음이 최근 연구에 의하여 밝혀지고 있다. 그러나 고려인삼 약리효능의 표적분자(target molecule)나 생화학적 작용기전(biochemical mechanism)이 세포 및 분자 수준에서 규명되지 못하여 고려인삼이 의약품으로 인정받지 못하고 건강식품으로 분류되고 있어 소비가 한인 흑인 히스패닉 시장에 한정되고 있고, 최근에는 타 경쟁국 인삼에 비해 수출 경쟁력이 약화되고 있는 실정이다. 본 연구에서는 고려인삼 추출물과 효능성분이 혈관내피세포 기능조절에 미치는 효능 및 작용기전을 규명하여 고려인삼이 호발성 혈관질환에 대한 예방 및 치료 효능이 있음을 분자 및 유전자 수준에서 확인하고자 하였다.

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Analysis Study on 32nd OPCW Proficiency Test Sample with GC-TSQ CI (GC-TSQ CI 분석법을 이용한 제32차 OPCW 숙련도 시험 시료 분석 연구)

  • Kim, Hyunsuk;Jung, Changhee;Lee, Yonghan
    • Journal of the Korea Institute of Military Science and Technology
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    • v.17 no.6
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    • pp.828-835
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    • 2014
  • GC-TSQ CI technique was applied for analysis of samples for the $32^{nd}$ OPCW proficiency test. Eight chemical weapon convention(CWC) related chemicals were identified by product ion mode analysis with GC-TSQ in the samples. Choice of specific precursor ion made it possible to supply selective total ion chromatograms(TICs) of target molecule. GC-TSQ CI anaylsis technique was useful method for chemical warfare agent verification because analysis selectivity was improved by choice of mother molecule as precursor ion and gave mass spectra.

On the Crystal Structure of a human Cell Division Cycle Controlling Protein Kinase(CDK2) and Structure-Based Drug Design

  • Kim, Sung-Hou-
    • Proceedings of the Korean Society of Applied Pharmacology
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    • pp.41-49
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    • 1994
  • The most common conventional method of discovering a drug involves a massive screening of a large number of compounds in chemical libraries or in the extracts from natural sources such as plants or microbial broths followed by chemical modification of one or more active compounds to improve their properties as a drug. When the three-dimensional structure of the target molecule for which the drug is searched is known the drug discovery process can be significantly simplified, This is especially true when the three-dimensional structure of a complex between the target and a lead compound is known. In this lecture our experience on the structure-based drug design for human CDK2(cyclin-dependent protein kinase 2) will be discussed with special emphasis on the strength and weakness of this approach of drug discovery. The regulation of the activity of CDK2 plays an important role in the cell proliferation of normal and cancer cells.

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Metabolic perturbation of an Hsp90 C-domain inhibitor in a lung cancer cell line, A549 studied by NMR-based chemometric analysis

  • Hur, Su-Jung;Lee, Hye-Won;Shin, Ai-Hyang;Park, Sung Jean
    • Journal of the Korean Magnetic Resonance Society
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    • v.18 no.1
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    • pp.10-14
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    • 2014
  • Hsp90 is a good drug target molecule that is involved in regulating various signaling pathway in normal cell and the role of Hsp90 is highly emphasized especially in cancer cells. Thus, much efforts for discovery and development of Hsp90 inhibitor have been continued and a few Hsp90 inhibitors targeting the N-terminal ATP binding site are being tested in the clinical trials. There are no metabolic signature molecules that can be used to evaluate the effect of Hsp90 inhibition. We previously found a potential C-domain binder named PPC1 that is a synthetic small molecule. Here we report the metabolomics study to find signature metabolites upon treatment of PPC1 compound in lung cancer cell line, A549 and discuss the potentiality of metabolomic approach for evaluation of hit compounds.

The Need for the Development of Pig Brain Tumor Disease Model using Genetic Engineering Techniques (유전자 조작기법을 통한 돼지 뇌종양 질환모델 개발의 필요성)

  • Hwang, Seon-Ung;Hyun, Sang-Hwan
    • Journal of Embryo Transfer
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    • v.31 no.1
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    • pp.97-107
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    • 2016
  • Although many diseases could be treated by the development of modern medicine, there are some incurable diseases including brain cancer, Alzheimer disease, etc. To study human brain cancer, various animal models were reported. Among these animal models, mouse models are valuable tools for understanding brain cancer characteristics. In spite of many mouse brain cancer models, it has been difficult to find a new target molecule for the treatment of brain cancer. One of the reasons is absence of large animal model which makes conducting preclinical trials. In this article, we review a recent study of molecular characteristics of human brain cancer, their genetic mutation and comparative analysis of the mouse brain cancer model. Finally, we suggest the need for development of large animal models using somatic cell nuclear transfer in translational research.