• Title/Summary/Keyword: target molecule

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Biosensors: a review (바이오센서)

  • Hwang, Kyo-Seon;Kim, Sang-Kyung;Kim, Tae-Song
    • Journal of Sensor Science and Technology
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    • v.18 no.4
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    • pp.251-262
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    • 2009
  • Biosensors exploit the specific binding between recognition molecule on the biosensor surface and target molecule in analyte and are used in the detection of specific biomolecules such as protein, DNA, cell, virus, etc., with a view towards developing analytical devices. Recently, application field of biosensors have been expanding from diagnosis to biodefense because they can basically serve as high performance devices. This review describes the basic information of biosensors including definition, classification, and operational principle. Moreover, we introduce micro/nano technology-based biosensors with better detection performance than traditional method and their application examples.

γ-Irradiation Induced Adhesion Molecules are Reduced by Vitamin C in Human Endothelial Cells

  • Son, Eun-Wha;Kim, Byung-Oh;Pyo, Suh-Kneung
    • Biomolecules & Therapeutics
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    • v.12 no.3
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    • pp.145-150
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    • 2004
  • Inflammation is a frequent radiation-induced reaction following therapeutic irradiation. Treatment of human umbilical endothelial cells (HUVEC) with ${\gamma}$-irradiation (${\gamma}$IR) induces the expression of adhesion proteins such as intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), and E-selectin. Since the upregulation of these proteins on endothelial cell Surface has been known to be associated with inflammation, interfering with the expression of adhesion molecules is an important therapeutic target. In the present study, we demonstrate that vitamin C inhibits ${\gamma}$IR induced expression of ICAM-1, VCAM-1, and E-selectin on HUVEC in a dose- and time dependent manner. Vitamin C a1so inhibited the production of Nitric oxide (NO) induced by ${\gamma}$IR. These data suggest that vitamin C has therapeutic potential for the treatment of various inflammatory disorder associated with an increase of endothelial leukocyte adhesion molecules.

Allicin reduces expression of Intercellular Adhesion Molecule-1 (ICAM-1) in gamma-irradiated endothelial cells: Involvement of p38 MAP kinase signalling pathway.

  • Son, Eun-Hwa;Mo, Sung-Ji;Cho, Seong-Jun;Yang, Kwang-Hee;Rhee, Dong-Kwon;Pyo, Suhk-Neung
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.307.1-307.1
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    • 2002
  • Inflammation is a frequent radiation-induced following therapeutic irradiation. Since the upregulation of adhesion molecules on endothelial cell surface has been known to be associated with inflammation. interfering with the expression of adhesion molecules is an important therapeutic target. We examined the effect of allicin. a major component of garlic. on the induction of intercellular adhesion molecule-1 (lCAM-1) by gamma-irradiation and the mechanisms of its effect in gamma-irradiated human umbilical vein endothelial cells (HUVECs). (omitted)

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새로운 퀴놀론 항균제의 합성

  • 강석구
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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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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Regulatory Role of the Serpin Strain

  • Seo, Eun-Joo;Yu, Myeong-Hee
    • Proceedings of the Korean Biophysical Society Conference
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    • 2002.06b
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    • pp.30-30
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    • 2002
  • The native forms of common globular proteins are in their most stable state but the native forms of plasma serpins (serine protease inhibitors) show high-energy state interactions. The high-energy state strain of a ${\alpha}$$_1$-antitrypsin, a prototype serpin, is distributed throughout the whole molecule, but the strain that regulates the function directly appears to be localized in the region where the reactive site loop is inserted during complex formation with a target protease.(omitted)

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Combinatorial Library and Chemogenomics Approach: Discovery of Protein Secondary Structure Mimetic Small Molecule Inhibitors of Tryptase and Ref-l for Asthma

  • Moon, Sung-Hwan
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.92-92
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    • 2003
  • The drug discovery landscape is changing rapidly in the post-genomic era. Mapping of the human genome has led to an abundance of potential drug targets. Drug discovery times and costs can be significantly reduced by developing methods for high throughput target identification/ validation, multiplexed assay development and high efficient combinatorial chemistry. (omitted)

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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.

Prediction of Binding Free Energy Calculation Using Molecular Mechanics/Poisson-Boltzmann Surface Area (MM-PBSA) Method in Drug Discovery: A Short Review

  • Kothandan, Gugan;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.5 no.4
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    • pp.216-219
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    • 2012
  • Structure-based drug design possibly benefit from in silico methods that precisely predict the binding affinity of small molecules to target macromolecules. There are many limitations arise from the difficulty of predicting the binding affinity of a small molecule to a biological target with the current scoring functions. There is thus a strong interest in novel methodologies based on MD simulations that claim predictions of greater accuracy than current scoring functions, helpful for a regular use designed for drug discovery in the pharmaceutical industry. Herein, we report a short review on free energy calculations using MMPBSA method a useful method in structure based drug discovery.

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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    • 1994.04a
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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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Chemical kinomics: a powerful strategy for target deconvolution

  • Kim, Do-Hee;Sim, Tae-Bo
    • BMB Reports
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    • v.43 no.11
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    • pp.711-719
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    • 2010
  • Kinomics is an emerging and promising approach for deciphering kinomes. Chemical kinomics is a discipline of chemical genomics that is also referred to as "chemogenomics", which is derived from chemistry and biology. Chemical kinomics has become a powerful approach to decipher complicated phosphorylation-based cellular signaling networks with the aid of small molecules that modulate kinase functions. Moreover, chemical kinomics has played a pivotal role in the field of kinase drug discovery as it enables identification of new molecular targets of small molecule kinase modulators and/or exploitation of novel functions of known kinases and has also provided novel chemical entities as hit/lead compounds. In this short review, contemporary chemical kinomics technologies such as activity-based protein profiling, T7 kinasetagged phages, kinobeads, three-hybrid systems, fluorescenttagged kinase binding assays, and chemical genomic profiling are discussed along with a novel allosteric Bcr-Abl kinase inhibitor (GNF-2/GNF-5) as a successful application of chemical kinomics approaches.