• Title/Summary/Keyword: $A_2$ inhibitor

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Numerical Study on the Effects of Surface-inhibitors on the Spontaneous Ignition of Coal Stockpile (저탄장 자연발화에 미치는 표면차단제 영향에 관한 수치 해석적 연구)

  • Kim, Jae-Kwan;Park, Seok-Un;Shin, Dong-ik
    • Fire Science and Engineering
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    • v.33 no.2
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    • pp.20-29
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    • 2019
  • In this paper, the effect of spontaneous combustion inhibitor on the surface of coal stockpile in coal yard was investigated by numerical analysis. First, the numerical analysis method of the present study was compared with the results of the previous study by analyzing the case where the spontaneous combustion inhibitor was not applied, and the effect of preventing spontaneous combustion by various areas and positions for spraying spontaneous combustion inhibitor was analyzed. As a result, the larger the application area of the spontaneous combustion inhibitor, the more the effect of preventing spontaneous combustion by blocking the oxygen inflow into the coal stockpile, and the greater the effect of the spontaneous combustion prevention when spraying spontaneous combustion inhibitor from the bottom of the coal stockpile. Spontaneous combustion inhibitor should be sprayed effectively, considering the economic aspects, such as manufacturing cost etc.

A Study on the Application to Anti-corrosive Film of Acryl Emulsion for the Reducing of Environmental Pollutants (환경유해물질 저감을 위한 Acryl emulsion의 방청필름 응용 연구)

  • Lee, S.H.
    • Corrosion Science and Technology
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    • v.8 no.5
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    • pp.197-202
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    • 2009
  • The high toxicity of wax, oil, varnish and volatile corrosion inhibitor(VCI) corrosion inhibitors lead to an increasing interest in using non-toxic alternatives such as anti-corrosive film. This study aims to investigate the possibility to use acryl based anti-corrosive film as a substitution of toxic corrosion inhibitors. Acryl emulsions were polymerized by several acryl monomers(acrylonitrile(AN), n-butyl acrylate(nBA), methylmethacrylate(MMA) and glycycyl methacrylate(GMA)), non-toxic corrosion inhibitor, crosslinking agents(diethylene glycol dimethacrylate(DEGDA)) and various additives in order to apply substrate of anti-corrosive film. Acryl emulsion for anti-corrosive film(AeACF) as a substrate of corrosion inhibitor film has excellent removal characteristic at above $25^{\circ}C$. The crosslinked by DEGDA in a range of above 4 wt% content anti-corrosive film can easily remove from the metal surface by using hands because it kept a balance of cohesion and adhesion strength. Anti - corrosive performance of AeACF is better than anti-corrosive oil by corrosion rate test, which was measured $54.3mg/dm^2$ day(MDD) and $142.9mg/dm^2$ day, respectively. Anti-corrosive film consisting of acryl monomers and inorganic anti-corrosive ingredients did not emit any toxic pollutants by gas chromatography. Thus it is estimated that acryl based anti-corrosion film can substitute toxic corrosion inhibitors.

PBT-6, a Novel PI3KC2γ Inhibitor in Rheumatoid Arthritis

  • Kim, Juyoung;Jung, Kyung Hee;Yoo, Jaeho;Park, Jung Hee;Yan, Hong Hua;Fang, Zhenghuan;Lim, Joo Han;Kwon, Seong-Ryul;Kim, Myung Ku;Park, Hyun-Ju;Hong, Soon-Sun
    • Biomolecules & Therapeutics
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    • v.28 no.2
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    • pp.172-183
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    • 2020
  • Phosphoinositide 3-kinase (PI3K) is considered as a promising therapeutic target for rheumatoid arthritis (RA) because of its involvement in inflammatory processes. However, limited studies have reported the involvement of PI3KC2γ in RA, and the underlying mechanism remains largely unknown. Therefore, we investigated the role of PI3KC2γ as a novel therapeutic target for RA and the effect of its selective inhibitor, PBT-6. In this study, we observed that PI3KC2γ was markedly increased in the synovial fluid and tissue as well as the PBMCs of patients with RA. PBT-6, a novel PI3KC2γ inhibitor, decreased the cell growth of TNF-mediated synovial fibroblasts and LPS-mediated macrophages. Furthermore, PBT-6 inhibited the PI3KC2γ expression and PI3K/AKT signaling pathway in both synovial fibroblasts and macrophages. In addition, PBT-6 suppressed macrophage migration via CCL2 and osteoclastogenesis. In CIA mice, it significantly inhibited the progression and development of RA by decreasing arthritis scores and paw swelling. Three-dimensional micro-computed tomography confirmed that PBT-6 enhanced the joint structures in CIA mice. Taken together, our findings suggest that PI3KC2γ is a therapeutic target for RA, and PBT-6 could be developed as a novel PI3KC2γ inhibitor to target inflammatory diseases including RA.

A Study about the Mechanism of $Ca^{2+}$ and Pi Homeostasis by Estradiol 17$\beta$ in Proximal Tubule Cells in the Osteoporosis

  • Han Ho-jae;Park Soo-Hyun
    • Biomedical Science Letters
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    • v.10 no.4
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    • pp.375-383
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    • 2004
  • It has been reported that osteoporosis induced by the deficiency of estrogens in menopause is associated with the unbalance of Ca/sup 2+/ and Pi levels. Proximal tubule is very important organ to regualte Ca/sup 2+/ and Pi level in the body. However, the effect of estrogens on Ca/sup 2+/ and Pi regulation was not elucidated. Thus, we examined the effect of 17-β estradiol (E₂) on Ca/sup 2+/ and Pi uptake in the primary cultured rabbit renal proxiaml tubule cells. In the present study, E₂(> 10/sup -9/M) decreases Ca/sup 2+/uptake and stimulates Pi uptake over 3 days. E₂-induced decrease of Ca/sup 2+/ uptake and stimulation of Pi uptake were blocked by actinomycin D (a gene transcription inhibitor), cycloheximide (a protein synthesis inhibitor). tamoxifen, and progesterone (estrogen receptor antagonists). E₂-induced decrease of Ca/sup 2+/ uptake and stimulation of Pi uptake were blocked by SQ22536 (an adenylate cyclase inhibitor), Rp-cAMP (a cAMP antagonist), and PKI (a protein kinase A inhibitor). Indeed, E₂ increased cAMP formation. In addition, E₂-induced decrease of Ca/sup 2+/ uptake and stimulation of Pi uptake were blocked by staurosporine, H-7, and bisindolylmaleimide I (protein kinase C inhibitors) and E₂ translocated PKC from cytoslic fraction to membrane fraction. In conclusion, E₂ decreased Ca/sup 2+/ uptake and stimulated Pi uptake via cAMP and PKC pathway in the PTCs.

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Mechanisms of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Resistance and Strategies to Overcome Resistance in Lung Adenocarcinoma

  • Chang, Yoon Soo;Choi, Chang-Min;Lee, Jae Cheol
    • Tuberculosis and Respiratory Diseases
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    • v.79 no.4
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    • pp.248-256
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    • 2016
  • Somatic mutations that lead to hyperactivation of epidermal growth factor receptor (EGFR) signaling are detected in approximately 50% of lung adenocarcinoma in people from the Far East population and tyrosine kinase inhibitors are now the standard first line treatment for advanced disease. They have led to a doubling of progression-free survival and an increase in overall survival by more than 2 years. However, emergence of resistant clones has become the primary cause for treatment failure, and has created a new challenge in the daily management of patients with EGFR mutations. Identification of mechanisms leading to inhibitor resistance has led to new therapeutic modalities, some of which have now been adapted for patients with unsuccessful tyrosine kinase inhibitor treatment. In this review, we describe mechanisms of tyrosine kinase inhibitor resistance and the available strategies to overcoming resistance.

Penicillium sp.-L4의 균성장 및 효소작용을 억제하는 $\beta$-glucosidase inhibitor의 분리 및 특성

  • Kim, Moo-Sung;Ha, Sung-Yoon;Jeon, Gi-Boong;Lim, Dal-Taek;Park, Byung-Hwa;Lee, Bo-Seop;Lee, Sang-Rin;Choi, Yong-Keel
    • Microbiology and Biotechnology Letters
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    • v.25 no.2
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    • pp.189-196
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    • 1997
  • A producer of inhibitor against ${\beta}-glucosidase$ of Penicillium sp.-L4 was screened from Actinomycetes, and the isolated strain was identified as Streptomyces sp. The inhibitor produced was very stable against heat, acidic and alkaline conditions, proteolytic and amylolytic enzymes. The inhibotor was purified from culture broth through activated carbon treatment, ultrafiltration, anion and cation exchange, activated carbon columm, acetone precipitation and preparative HPLC. It showed inhibitory activities against a variety of dissacharide hydrolyzing enzymes produced by P.sp.-L4, and the mode of inhibition was competitive. Its structure and molecular formular was elucidated by IR, $^1H\;and\;^{13}C$ NMR and FAB/Mass spectrometry, which was identified as 1-deoxynojirimycin (dNM). dNM showed inhibitory effects on the cell growth and hydrolytic enzyme action of P.sp.-L4 on agar plate and infected lemon peel.

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Production of Antihypertensive Angiotensin I-Converting Enzyme Inhibitor from Malassezia pachydermatis G-14

  • Jeong, Seung-Chan;Kim, Jae-Ho;Kim, Na-Mi;Lee, Jong-Soo
    • Mycobiology
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    • v.33 no.3
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    • pp.142-146
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    • 2005
  • To produce a novel antihypertensive angiotensin I-converting enzyme (ACE) inhibitor from yeast, a yeast isolate, designated G-14 showing the highest ACE inhibitory activity was obtained and identified as Malassezia pachydermatis based on morphological, biochemical and cultural characteristics. The maximal extracellular ACE inhibitor production was obtained from M. pachydermatis G-14 when the strain was cultured in YEPD medium containing 0.5% yeast extract, 3.0% peptone and 2.0% glucose at $30^{\circ}C$ for 24 h and the final ACE inhibitory activity was 48.9% under the above condition.

Madurahydroxylactone, an Inhibitor of Staphylococcus aureus FtsZ from Nonomuraea sp. AN100570

  • Kim, Bo-Min;Choi, Ha-Young;Kim, Geon-Woo;Zheng, Chang-Ji;Kim, Young-Ho;Kim, Won-Gon
    • Journal of Microbiology and Biotechnology
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    • v.27 no.11
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    • pp.1994-1998
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    • 2017
  • FtsZ, a bacterial cell-division protein, is an attractive antibacterial target. In the screening for an inhibitor of Staphylococcus aureus FtsZ, madurahydroxylactone (1) and its related derivatives 2-5 were isolated from Nonomuraea sp. AN100570. Compound 1 inhibited S. aureus FtsZ with an $IC_{50}$ of $53.4{\mu}M$ and showed potent antibacterial activity against S. aureus and MRSA with an MIC of $1{\mu}g/ml$, whereas 2-5 were weak or inactive. Importantly, 1 induced cell elongation in the cell division phenotype assay, whereas 2-5 did not. It indicates that 1 exhibits its potent antibacterial activity via inhibition of FtsZ, and the hydroxyl group and hydroxylactone ring of 1 are critical for the activity. Thus, madurahydroxylactone is a new type of inhibitor of FtsZ.

Production of an Anti-dementia Butyrylcholinesterase Inhibitor from Non-pathogenic Wild Yeast, Saccharomyces cerevisiae WJSL 0113 (비병원성 야생효모 Saccharomyces cerevisiae WJSL 0113으로부터 항치매성 Butyrylcholinesterase 저해물질의 생산)

  • Han, Sang-Min;Park, Seon-Jeong;Jang, Ji-Eun;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.49 no.2
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    • pp.243-248
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    • 2021
  • In this study, screening of potent non-pathogenic wild yeast with high anti-dementia butyrylcholinesterase (BChE) inhibitory activity and production condition of a BChE inhibitor were described. Among 36 non-pathogenic wild yeasts, Saccharomyces cerevisiae WJSL 0113 showed the highest BChE inhibitory activity of 85.2%. The specific BChE inhibitor was maximally produced when S. cerevisiae WJSL 0113 was cultured at 30℃ for 48 h in a yeast extract-peptone-dextrose medium.

Modulation of L-type $Ca^{2+}$ Channel Currents by Various Protein Kinase Activators and Inhibitors in Rat Clonal Pituitary $GH_3$ Cell Line

  • Bae, Young-Min;Baek, Hye-Jung;Cho, Ha-Na;Earm, Yung-E;Ho, Won-Kyung
    • The Korean Journal of Physiology and Pharmacology
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    • v.5 no.2
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    • pp.139-146
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    • 2001
  • L-type $Ca^{2+}$ channels play an important role in regulating cytosolic $Ca^{2+}$ and thereby regulating hormone secretions in neuroendocrine cells. Since hormone secretions are also regulated by various kinds of protein kinases, we investigated the role of some kinase activators and inhibitors in the regulation of the L-type $Ca^{2+}$ channel currents in rat pituitary $GH_3$ cells using the patch-clamp technique. Phorbol 12,13-dibutyrate (PDBu), a protein kinase C (PKC) activator, and vanadate, a protein tyrosine phosphatase (PTP) inhibitor, increased the $Ba^{2+}$ current through the L-type $Ca^{2+}$ channels. In contrast, bisindolylmaleimide I (BIM I), a PKC inhibitor, and genistein, a protein tyrosine kinase (PTK) inhibitor, suppressed the $Ba^{2+}$ currents. Forskolin, an adenylate cyclase activator, and isobutyl methylxanthine (IBMX), a non-specific phosphodiesterase inhibitor, reduced $Ba^{2+}$ currents. The above results show that the L-type $Ca^{2+}$ channels are activated by PKC and PTK, and inhibited by elevation of cyclic nucleotides such as cAMP. From these results, it is suggested that the regulation of hormone secretion by various kinase activity in $GH_3$ cells may be attributable, at least in part, to their effect on L-type $Ca^{2+}$ channels.

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