• Title/Summary/Keyword: Small molecule

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Cloning, Sequencing and Characterization of Mitochondrial Control Region of the Domestic Silkwom, Bombyx mori

  • Lee, Jin-Sung;Kim, Ki-Hwan;Hoe, Hyang-Sook;Park, Jae-Heung;Kang, Seok-Woo;Lee, Sang-Han;Hwang, Jae-Sam
    • International Journal of Industrial Entomology and Biomaterials
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    • v.2 no.1
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    • pp.87-89
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    • 2001
  • The nucleotide sequence of the domestic silkworm (Bombyx mori) mitochondrial (mt) control region and its flanking genes was determined from PCR clones. The control region of the silkworm mt genome was located between the small ribosomal RNA gene and transfer RN $A^{Met}$. This 499 bp control region hale 95.4% A+T content. Extensive comparative analysis studies performed with similar control region of other insect genomes could not reveal a highly conserved region containing conserved motifs of animal mito-chondrial genome. The remarkable feature that found in this control region was the presence of tandem motifs containing nine repetitive sequences. The potential usefulness of this motif sequences for Bombyx species or their taxonomically related species is enhanced by its unique localization in the maternally inheritance mitochondrial molecule.e.

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Recent progress in aromatic radiofluorination

  • Kwon, Young-Do;Chun, Joong-Hyun
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.5 no.2
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    • pp.145-151
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    • 2019
  • Fluorine-18 is considered to be the radionuclide of choice for positron emission tomography (PET). Thus, the development of small molecule-based radiopharmaceuticals for use in diagnostic imaging relies heavily on efficient radiofluorination techniques. Until the early 2000s, diaryliodonium salts and aryliodonium ylides were widely employed as labeling precursors to yield aromatic PET radiotracers with cyclotron-produced [18F]fluoride ion. Rapid recent progress in the development of efficient borylation methods has led to a paradigm shift in 18F-labeling methods. In addition, deoxyfluorination has attracted a great deal of interest as an alternative approach to aryl ring activation with 18F-. In this review, methods for radiolabel development are discussed with a specific focus on the progress made in the last 5 years. Other interesting 18F-based protocols are also briefly introduced. New methods for exploiting 18F- are expected to increase the number of 18F-labeling methods, to allow applications in a range of chemical environments.

Stress Responses through Heat Shock Transcription Factor in S. cerevisiae

  • Hahn, Ji-Sook;Hu, Zhanzhi;Thiele, Dennis J.;Lyer, Vishwanath R.
    • Proceedings of the Microbiological Society of Korea Conference
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    • 2005.05a
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    • pp.105-109
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    • 2005
  • Heat Shock Transcription Factor (HSF), and the promoter heat Shock Element (HSE), are among the most highly conserved transcriptional regulatory elements in nature. HSF mediates the transcriptional response of eukaryotic cells to heat, infection and inflammation, pharmacological agents, and other stresses. While HSF is essential for cell viability in yeast, oogenesis and early development in Drosophila, extended life-span in C. elegans, and extra-embryonic development and stress resistance in mammals, little is known about its full range of biological target genes. We used whole genome analyses to identify virtually all of the direct transcriptional targets of yeast HSF, representing nearly three percent of the genomic loci. The majority of the identified loci are heat-inducibly bound by yeast HSF, and the target genes encode proteins that have a broad range of biological functions including protein folding and degradation, energy generation, protein secretion, maintenance of cell integrity, small molecule transport, cell signaling, and transcription. Approximately 30% of the HSF direct target genes are also induced by the diauxic shift, in which glucose levels begin to be depleted. We demonstrate that phosphorylation of HSF by Snf1 kinase is responsible for expression of a subset of HSF targets upon glucose starvation.

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Characteristics of Organic Thin Film Transistors with Organic and Organic-inorganic Hybrid Polymer Gate Dielectric (유기물과 유무기 혼합 폴리머 게이트 절연체를 사용한 유기 박막 트랜지스터의 특성)

  • Bae, In-Seob;Lim, Ha-Young;Cho, Su-Heon;Moon, Song-Hee;Choi, Won-Seok
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.22 no.12
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    • pp.1009-1013
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    • 2009
  • In this study, we have been synthesized the dielectric layer using pure organic and organic-inorganic hybrid precursor on flexible substrate for improving of the organic thin film transistors (OTFTs) and, design and fabrication of organic thin-film transistors (OTFTs) using small-molecule organic semiconductors with pentacene as the active layer with record device performance. In this work OTFT test structures fabricated on polymerized substrates were utilized to provide a convenient substrate, gate contact, and gate insulator for the processing and characterization of organic materials and their transistors. By an adhesion development between gate metal and PI substrate, a PI film was treated using $O_2$ and $N_2$ gas. The best peel strength of PI film is 109.07 gf/mm. Also, we have studied the electric characteristics of pentacene field-effect transistors with the polymer gate-dielectrics such as cyclohexane and hybrid (cyclohexane+TEOS). The transistors with cyclohexane gate-dielectric has higher field-effect mobility, $\mu_{FET}=0.84\;cm^2/v_s$, and smaller threshold voltage, $V_T=-6.8\;V$, compared with the transistor with hybrid gate-dielectric.

Current state and prospective of the Korean medical research on the cancer metabolism (암특이적 대사에 대한 한의학적 연구의 현황 및 전망)

  • Chung, Tae-Wook;Kim, Eun-Yeong;Choi, Hee-Jin;Choi, Hee-Jung;Ha, Ki-Tae
    • Journal of Korean Traditional Oncology
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    • v.20 no.1
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    • pp.81-88
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    • 2015
  • Generally, normal cells synthesize adenosine triphosphate (ATP) through oxidative phosphorylation in the mitochondria. However, they produce ATP through lactic acid fermentation on hypoxic condition. Interestingly, many cancer cells rely on aerobic glycolysis for ATP generation instead of mitochondrial oxidative phosphorylation, which is termed as "Warburg effect". According to results from recent researches on differences of cancer cell metabolism from normal cell metabolism and because chemotherapy to suppress rapidly growing cells, as a side effect of cancer treatment, can still target healthy cells, there is merit in the development of small-molecule inhibitors targeting metabolic enzymes such as pyruvate dehydrogenase kinase (PDHK), lactate dehydrogenase (LDH) and monocarboxylate transporter (MCT). For new anticancer therapy, in this review, we show recent advances in study on cancer cell metabolism and molecules targeting metabolic enzymes which are importantly associated with cancer metabolism for cancer therapy. Furthermore, we would also like to emphasize the necessity of development of molecules targeting metabolic enzymes using herbal medicines and their constituents for anticancer drugs.

Identification of a novel type of small molecule inhibitor against HIV-1

  • Kim, Byung Soo;Park, Jung Ae;Kim, Min-Jung;Kim, Seon Hee;Yu, Kyung Lee;You, Ji Chang
    • BMB Reports
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    • v.48 no.2
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    • pp.121-126
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    • 2015
  • Here we report a new chemical inhibitor against HIV-1 with a novel structure and mode of action. The inhibitor, designated as A1836, inhibited HIV-1 replication and virus production with a 50% inhibitory concentration ($IC_{50}$) of $2.0{\mu}M$ in an MT-4 cell-based and cytopathic protection antiviral assay, while its 50% cytotoxic concentration ($CC_{50}$) was much higher than $50{\mu}M$. Examination of the effect of A1836 on in vitro HIV-1 reverse transcriptase (RT) and integrase showed that neither were molecular targets of A1836. The characterization and re-infection assay of the HIV-1 virions generated in the presence of A1836 showed that the synthesis of early RT products in the cells infected with the virions was inhibited dose-dependently, due in part to abnormal protein formation within the virions, thus resulting in an impaired infectivity. These results suggest that A1836 might be a novel candidate for the development of a new type of HIV-1 inhibitor.

Glycosylation of Flavonoids with E. coli Expressing Glycosyltransferase from Xanthomonas campestris

  • Kim, Jeong-Ho;Kim, Bong-Gyu;Kim, Jae-Ah;Park, Young-Hee;Lee, Yoon-Jung;Lim, Yoong-Ho;Ahn, Joong-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.17 no.3
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    • pp.539-542
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    • 2007
  • Glycosyltransferase family 1 (UOT) uses small chemicals including phenolics, antibiotics, and alkaloids as substrates to have an influence in biological activities. A glycosyltransferase (XcGT-2) from Xanthomonas campestris was cloned and consisted of a 1,257 bp open reading frame encoding a 45.5 kDa protein. In order to use this for the modification of phenolic compounds, XcGT-2 was expressed in Escherichia coli as a glutathione S-transferase fusion protein. With the E. coli transformant expressing XcGT-2, biotransformation of flavonoids was carried out. Flavonoids having a double bond between carbons 2 and 3, and hydroxyl groups at both C-3' and C-4', were glycosylated and the glycosylation position was determined to be at the hydroxyl group of C-3', using nuclear magnetic resonance spectroscopy. These results showed that XcGT-2 regiospecifically transferred a glucose molecule to the 3'-hydroxyl group of flavonoids containing both 3' and 4'-hydroxyl groups.

Cinnamic Acid Derivatives I, The Kinetics and Mechanism of the Hydrolysis and Synthesis of Cinnamanilide Derivatives (신남산 유도체 I, Cinnamanilide 유도체의 가수분해 메카니즘과 반응속도론적 연구)

  • Lee, Ki-Chang;Hwang, Yong-Hyun;Lee, Kwang-Il;Jung, Taek-Suh;Park, Kwang-Ha
    • Journal of the Korean Applied Science and Technology
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    • v.6 no.2
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    • pp.59-65
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    • 1989
  • The rate constants of the hydrolysis of cinnamanilide derivatives were determined UV spectrometry in $H_2SO_4\;(5{\sim}20N)$, NaOH($5{\sim}11N)\;at\;50{\sim}110^{\circ}C$ and rate equation could be applied over a strong acid and strong base were obtained. Final product of the hydrolysis was a cinnamic acid. The ${\rho}$ values obtained from the slope of linear plots of log $k_{abs}$ vs. Hammet $t{\sigma}$ constants were slightly negatives, Substituents on cinnamanilide showed a relatively small effect, with hydrolysis facilitated be electron donating group. Activation energy(Ea)was also calculated for the hydrolysis of the cinnamanilide. From this reaction rate equation, substituent effect and experimental of rate constants, that the hydrolysis of cinnamanillde was Initiated by the netural molecule of $H_2O$ which do not dissociate at strong acid, and proceeded by hydroxide ion at strong base.

Effect of Pressure on Catalytic Properties of Glutamate Racemase from Aquifex pyrophilus, an Extremophilic Bacteria

  • Lee, Ki-Seog;Chi, Young-Min;Yu, Yeon-Gyu
    • Journal of Microbiology and Biotechnology
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    • v.12 no.1
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    • pp.149-152
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    • 2002
  • The effect of pressure on the catalytic properties of glutamate racemase from Aquifex pyrophilus, an extremophilic bacterium, was investigated. The activation volume for the overall reaction $({\Delta}V^{\neq})$ and catalysis $({{Delta}V_{cat}}^{\neq})$ was -96.97 ml/mol and 4.97 ml/mol, respectively, while the reaction volume for the substrate binding (${\Delta}V_{K_m^-1}$) was -101.94 ml/mol. The large negative ${\Delta}V^{\neq}$ for the overall reaction indicated that the pressurization of glutamate racemase resulted in enhanced catalytic efficiencies. In addition, this value was also due to the large negative ${Delta}V_{K_m^-1}$ for the substrate binding. The negative value of ${Delta}V_{K_m^-1}$ implied that the conformational changes in the enzyme molecule occurred during the substrate binding process, thereby increasing the degree of hydration. The small value of ${{Delta}V_{cat}}^{\neq}$suggested that the pressure did not affect the glutamate racemase catalysis after the substrate binding.

Cadmium Altered Gene Expression Related to Zinc Homeostasis in the Mouse Brain (카드뮴이 마우스 뇌에서 아연의 항상성에 관여하는 유전자발현에 미치는 영향)

  • Park Jong-An;Yoe Eun-Young;Nam Sang-Hun;Jang Bong-Ki;Lee Jong-Wha;Kim Wan-Jong
    • Environmental Analysis Health and Toxicology
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    • v.19 no.4
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    • pp.389-399
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    • 2004
  • Metallothionein (MT), a small protein molecule which can bind or release metal ions, is involved in the regulation of cellular metal homeostasis. This study was investigated the accumulation of cadmium in blood, tissue (liver, kidney and brain), and the effect of cadmium on several key genes (MT-I, MT-II, ZnT-1) in zinc metabolism in the mouse. Mouses weighing 20∼25 g were randomly assigned to control and cadmium treated group (Cd group). Cd group was intraperitoneally injected with cadmium 2, 4, 8 mg/kg and control group was administerd with saline. Mouses of each group were sacrificed by decapitation 4 hours after the administration of cadmium. Cadmium contents in blood, liver, kidney and brain were increased by a dose-dependent manner. Accumulation of cadmium was mainly occurred in liver and kidney. Induction of MT-I and MT-II protein was increased, but ZnT-1 expression was decreased in a dose-dependent manner by the treatment of 2∼8 mg/kg cadmium. These results suggested that cadmium can be transported to brain and alter the expression of several key genes in zinc homeostasis.