• Title/Summary/Keyword: Small organic molecules

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A Novel 3-(8-Chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl Acetate Skeleton and Pharmacophore Model as Glucagon-like Peptide 1 Receptor Agonists

  • Gong, Young-Dae;Cheon, Hyae-Gyeong;Lee, Tae-Ho;Kang, Nam-Sook
    • Bulletin of the Korean Chemical Society
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    • v.31 no.12
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    • pp.3760-3764
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    • 2010
  • We screened 10,000 heterocyclic small molecules and identified a novel hit core skeleton of 3-(8-chloro-6-(trifluoromethyl) imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives. It has been selected as a potential glucagon-like peptide 1 receptor (GLP-1R) activator and demonstrated its effects in increasing GLP-1 secretion, and thereby increasing the glucose responsiveness in both in vitro and pharmacology analyses. Further studies are currently underway to optimize the potency and selectivity of 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate derivatives (hit compounds 2 and 8), and address their in vivo efficacy and therapeutic potential. These molecules may serve as useful evidence showing that compounds with a 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-yl)phenyl acetate moiety are selective GLP-1R agonists, and have potential as anti-diabetic treatment agents.

Organic matrix-free imaging mass spectrometry

  • Kim, Eunjin;Kim, Jisu;Choi, Inseong;Lee, Jeongwook;Yeo, Woon-Seok
    • BMB Reports
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    • v.53 no.7
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    • pp.349-356
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    • 2020
  • Mass spectrometry (MS) is an ideal tool for analyzing multiple types of (bio)molecular information simultaneously in complex biological systems. In addition, MS provides structural information on targets, and can easily discriminate between true analytes and background. Therefore, imaging mass spectrometry (IMS) enables not only visualization of tissues to give positional information on targets but also allows for molecular analysis of targets by affording the molecular weights. Matrix-assisted laser desorption/ionization-time of flight (MALDI-TOF) MS is particularly effective and is generally used for IMS. However, the requirement for an organic matrix raises several limitations that get in the way of accurate and reliable images and hampers imaging of small molecules such as drugs and their metabolites. To overcome these problems, various organic matrix-free LDI IMS systems have been developed, mostly utilizing nanostructured surfaces and inorganic nanoparticles as an alternative to the organic matrix. This minireview highlights and focuses on the progress in organic matrix-free LDI IMS and briefly discusses the use of other IMS techniques such as desorption electrospray ionization, laser ablation electrospray ionization, and secondary ion mass spectrometry.

Blue Organic Light Emitting triodes with Carbazole Based Small Molecules

  • Park, Jong-Wook;Kim, Dong-Hyun
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2001.07a
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    • pp.228-230
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    • 2001
  • We synthesized Bis(3-N-ethylcarbazolyl) terephthalidene(BECP) and Bis(3-7-ethyl-carbazolyl) cyanoterephthalidene(BECCP) and characterized EL properties of these materials. Our device shows a strong blue emission at 472 nm with a luminance efficiency of 0.9 lm/W at a voltage, a current density, and a brightness of 8 V, 5.7 mA/cm$^2$, and 130 cd/m$^2$, respectively.

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Blue Organic Light Emitting Diodes with Carbazole Based Small Molecules

  • Park, Jong-Wook;Woo, Hyung-Suk;Caroll, David;Lee, Ji-Hoon
    • 한국정보디스플레이학회:학술대회논문집
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    • 2001.08a
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    • pp.157-158
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    • 2001
  • We synthesized Bis(3-N-ethylcarbazolyl) terephthalidene(BECP) and Bis(3-N-ethylcarbazolyl) cyanoterephthalidene (BECCP) and characterized EL properties of these materials. Our device shows a strong blue emission at 472 nm with a luminance efficiency of 0.9 lm/Wat a voltage, a current density. and a brightness of 8 V, 5.7 $mA/cm^2$, and 130 $cd/m^2$, respectively.

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Optical Simulation for High Efficiency OLEDs

  • Jung, Boo-Young;Jung, Sung-Goo;HwangBo, Chang-Kwon
    • 한국정보디스플레이학회:학술대회논문집
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    • 2006.08a
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    • pp.966-969
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    • 2006
  • An optical model based on the optical thin-film theory is derived to calculate the output radiance of small molecules organic light-emitting diodes (OLEDs). We have designed the high efficiency OLEDs using the reflectance phase control of dielectric layers. It is found that OLED with a single $TiO_2$ dielectric layer is a good candidate to enhance the outcoupling efficiency and increase the color purity.

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Discovery of Novel RNA Targets Using Chemical Genomics

  • Yu, Jae-Hoon
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.93-93
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    • 2003
  • RNA plays an important role in numerous biological processes but little is known about the interactions between small organic molecules and RNA. Our previous work has shown that the heterodimeric compound designed by conjugation with neomycin and loop-specific chemical bind to the stem-loop structured RNA motifs. In the present study, heterodimer was used, in a reverse way, as a probe to identify structured RNA motifs. (omitted)

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Regulation of NFAT Activation: a Potential Therapeutic Target for Immunosuppression

  • Lee, Mina;Park, Jungchan
    • Molecules and Cells
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    • v.22 no.1
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    • pp.1-7
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    • 2006
  • The NFAT family of transcription factors plays pivotal roles in the development and function of the immune system. Their activation process is tightly regulated by calcium-dependent phosphatase calcineurin and has been a target of the immunosuppressive drugs cyclosporin A and FK-506. Although the clinical use of these drugs has dramatically increased the success of organ transplantation, their therapeutic use is limited by severe side effects. Recent studies for the calcineurin/NFAT signaling pathway have identified a number of cellular proteins that inhibit calcineurin function. Specific peptide sequences that interfere with the interaction between calcineurin and NFAT have also been characterized. Moreover, diverse approaches to identify small organic molecules that modulate NFAT function have been performed. This review focuses on the recent advances in our understanding of the inhibitory modulation of NFAT function, which may open up the additional avenues for immunosuppressive therapy.

Back-Extraction Processes of C.C.Lipase with Mediated AOT Reverse Micellar System

  • Lee, Sung-Sik;Kim, Bong-Gyu;Sung, Nak-Chang;Lee, Jong-Pal
    • Bulletin of the Korean Chemical Society
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    • v.25 no.6
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    • pp.873-877
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    • 2004
  • The relationship between the behaviors of c.c.lipase back-extraction and their percolation phenomena by using AOT reverse micellar systems (RVMS) has been studied by the addition of a small amount of additives to organic phase such as thiols and nonionic-surfactants focusing on micelle-micelle interactions. The values of ${\beta}_t$ defined by the variation of percolation processes and back-extraction behaviors of c.c.lipase have a good linear correlation. The hydrophobicity of additive molecules suppressing the cluster formation of reverse micelles (high values of ${\beta}_t$) improved the back-extraction behavior of c.c.lipase. The back-extraction fraction and its rate of c.c.clipase are increased with decreasing of the value of hydrophilic lipophilic balance (HLB) and increasing of the hydrophobicity per additive molecules added to reverse micellar systems (RVSM) in the same additives concentration.

Gold Nanostructure-Based Laser Desorption/Ionization Time-of-Flight Mass Spectrometry for Analysis of Small Biomolecules

  • Hye-Sun Cho;Tae Hoon Seo;Ji Hun Park;Young-Kwan Kim
    • Mass Spectrometry Letters
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    • v.15 no.1
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    • pp.26-39
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    • 2024
  • Gold nanostructures (Au NSs) are useful and interesting matrices for mass spectrometric analysis of various biomolecules based on organic matrix-free laser desorption/ionization time-of-flight mass spectrometry (LDI-TOF-MS). Au NSs provide high efficiency and versatility in LDI-TOF-MS analysis based on their well-established synthesis and surface functionalization, large surface area, high laser absorption capacity, and photothermal conversion efficiency. Therefore, Au NSs based LDI-TOF-MS can be a facile, functional, and efficient analytical method for important small biomolecules owing to its simple preparation, rapid analysis, salt-tolerance, signal reproducibility, and quantitative analysis. This review chronologically summarizes the important advance of Au NSs-based LDI-TOF-MS platforms in terms of in-depth mechanism, signal enhancement, quantitative analysis, and disease diagnosis.

Behaviors of Externally-Stimulated Organic Ultra Thin Films of Fatty Acid Halides (지방산 할로겐화물 유기초박막의 외부자극에 의한 거동)

  • Park, Keun-Ho;Lee, Jun-Ho;Kim, Duck-Sool
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.1
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    • pp.102-108
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    • 2009
  • Behaviors of saturated fatty acid halides (CI4, C16, C18) were measured by LB method when the molecules were stimulated by pressure. The saturated fatty acid halides were deposited on the indium tin oxide(lTO) glass by the LB method. The average organic ultra thin film size and the surface roughness of the fatty acid halides thin films were investigated using AFM. It was found that AFM images show small surface roughness ($2.5{\sim}5.0\;nm$) and the organic ultra thin film size of $2.5{\sim}12\;nm$. Both aggregations and pin-holes were also seen on the AFM images. However we found that the surface roughness. These effects seem to be reasonable to be related to the increase of the organic ultra thin film size of fatty acid halides.