• Title/Summary/Keyword: }inhibitor$

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Transcriptome analysis of iBET-151, a BET inhibitor alone and in combination with paclitaxel in gastric cancer cells

  • Kang, Sun Kyoung;Bae, Hyun Joo;Kwon, Woo Sun;Che, Jingmin;Kim, Tae Soo;Chung, Hyun Cheol;Rha, Sun Young
    • Genomics & Informatics
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    • v.18 no.4
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    • pp.37.1-37.11
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    • 2020
  • BET inhibitor, as an epigenetic regulator inhibitor, reduces the expression of oncogenes such as Myc and Bcl-2, which affects cancer growth and development. However, it has modest activity because of the narrow therapeutic index. Therefore, combination therapy is necessary to increase the anti-tumor effect. Paclitaxel, an anti-mitotic inhibitor, is used as second-line therapy for gastric cancer (GC) as a monotherapy or combination. In this study, we performed RNA sequencing of GC cells treated with iBET-151 and/or paclitaxel to identify the differentially expressed genes associated with possible mechanisms of synergistic effect. We also performed Gene Ontology enrichment and Kyoto Encyclopedia of Genes and Genomes pathway analyses to determine the most enriched terms and pathways of upregulated and downregulated genes. We found 460 genes in which iBET-151 and paclitaxel combination treatment changed more than single-treatment or no-treatment. Thus, additional functional studies are needed, but our results provide the first evidence of the synergistic effect between iBET-151 and paclitaxel in regulating the transcriptome of GC cells.

Solution Conformations of the Substrates and Inhibitor of Hepatitis C Virus NS3 Protease

  • 이정훈;방근수;정진원;안인애;노성구;이원태
    • Bulletin of the Korean Chemical Society
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    • v.20 no.3
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    • pp.301-306
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    • 1999
  • Hepatitis C virus (HCV) has been known to be an enveloped virus with a positive strand RNA genome and the major agent of the vast majority of transfusion associated cases of hepatitis. For viral replication, HCV structural proteins are first processed by host cell signal peptidases and NS2/NS3 site of the nonstructural protein is cleaved by a zinc-dependent protease NS2 with N-terminal NS3. The four remaining junctions are cleaved by a separate NS3 protease. The solution conformations of NS4B/5A, NS5A/5B substrates and NS5A/5B inhibitor have been determined by two-dimensional nuclear magnetic resonance (NMR) spectroscopy. NMR data suggested that the both NS5A/5B substrate and inhibitor appeared to have a folded tum-like conformation not only between P1 and P6 position but also C-terminal region, whereas the NS4B/5A substrate exhibited mostly extended conformation. In addition, we have found that the conformation of the NS5A/5B inhibitor slightly differs from that of NS5A/5B substrate peptide, suggesting different binding mode for NS3 protease. These findings will be of importance for designing efficient inhibitor to suppress HCV processing.

Evaluation of the Inhibitive Performance of Cyperus Conglomeratus Leaves Extract as a Green Corrosion Inhibitor on Mild Steel XC70 in Acid Medium

  • Belkis, Guessoum;Abdelkader, Hadj Seyd;Oumelkheir, Rahim
    • Corrosion Science and Technology
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    • v.21 no.3
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    • pp.171-183
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    • 2022
  • The performance and inhibitory action of the aqueous extract of Cyperus Conglomeratus's leaves against corrosion of XC70 steel in a 1M HCl acid medium are studied by the determination of the weight loss, the potentiodynamic polarization curves analysis, and electrochemical impedance measurements (electrochemical techniques). The corrosion inhibitory efficiency of XC70 steel increases with the increasing concentration of the green inhibitor, however, the corrosion rate of the steel decreases. Weight loss measurements show that the maximum percentage corrosion inhibition efficiency is approximately 61.86%, while the analysis of the mixed character polarization curves shows that the inhibitor could achieve an inhibition efficiency of 86.96%. The electrochemical impedance study confirmed that the value of the charge transfer resistance (Rct) increases and the value of the double layer capacity (Cdl) decreases with increasing concentration of the aqueous extract of Cyperus Conglomeratus's leaves, thus increasing the inhibition efficiency. The study showed that this aqueous extract acts by adsorption on the metal surface; this adsorption follows the Langmuir isotherm. This research work showed that Cyperus Conglomeratus leaves extract acts as an effective and eco-friendly inhibitor on mild steel in an acid medium.

Use of Capparis decidua Extract as a Green Inhibitor for Pure Aluminum Corrosion in Acidic Media

  • Al-Bataineh, Nezar;Al-Qudah, Mahmoud A.;Abu-Orabi, Sultan;Bataineh, Tareq;Hamaideh, Rasha S.;Al-Momani, Idrees F.;Hijazi, Ahmed K.
    • Corrosion Science and Technology
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    • v.21 no.1
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    • pp.9-20
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    • 2022
  • The aim of this paper is to study corrosion inhibition of Aluminum with Capparis decidua extract. The study was performed in a 1.0 M solution of hydrochloric acid (HCl) and was monitored both by measuring mass loss and by using electrochemical and polarization methods. A scanning electron microscopy (SEM) technique was also applied for surface morphology analysis. The results revealed high inhibition efficiency of Capparis decidua extract. Our data also determined that efficiency is governed by temperature and concentration of extract. Optimum (88.2%) inhibitor efficiency was found with maximum extract concentration at 45 o C. The results also showed a slight diminution of aluminum dissolution when the temperature is low. Based on the Langmuir adsorption model, Capparis decidua adsorption on the aluminum surface shows a high regression coefficient value. From the results, the activation enthalpy (∆H#) and activation entropy (∆S#) were estimated and discussed. In conclusion, the study clearly shows that Capparis decidua extract acted against aluminum corrosion in acidic media by forming a protective film on top of the aluminum surface.

Inhibition Effect of Nevirapine an Antiretroviral on the Corrosion of Mild Steel Under Acidic Condition

  • Bhat, J. Ishwara;Alva, Vijaya D.P.
    • Journal of the Korean Chemical Society
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    • v.55 no.5
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    • pp.835-841
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    • 2011
  • Corrosion inhibition of mild steel by nevirapine, an antiretroviral has been investigated using potentiodynamic polarization, electrochemical impedance spectroscopy technique and weight loss methods. The experimental results suggested, nevirapine is a good corrosion inhibitor for mild steel in 1M hydrochloric acid medium and the inhibition efficiency increased with increase in inhibitor concentration. The kinetic parameters for corrosion process and thermodynamic parameters for adsorption process were calculated and discussed. The adsorption of the inhibitor on the surface of mild steel followed Langmuir adsorption isotherm.

The Development of Repair System for RC Members with Damaged by Rebar Corrosion Using Inhibitor with High Nitrite Content (아초산계 방청제 도포에 의한 철근 부식 보수 시스템 공법 개발)

  • 이한승;나정일;박순만
    • Proceedings of the Korea Concrete Institute Conference
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    • 2001.05a
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    • pp.359-364
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    • 2001
  • The purpose of this study is to develop the repair system for RC members with damaged by rebar corrosion using new corrosion inhibitor which was high nitrite content. In the experiments, the acceleration corrosion test of rebar was conducted using the specimen which was applied by various repair system. As a result, it was confirmed that the new repair system without concrete patching had high anti-corrosion property compared with other repair systems and was very effective as a spray type corrosion inhibitor in concrete containing chloride (0.1% of NaCl).

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Effects of Trypsin Inhibitors on Oleic acid Induced Acute Pancreatitis in Dogs (개에서 Oleic acid로 유발시킨 급성췌장염에 대한 Trypsin inhibitor의 투여효과)

  • 윤영민;최희인;조명행
    • Biomolecules & Therapeutics
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    • v.5 no.2
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    • pp.158-164
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    • 1997
  • To investigate the effects of trypsin inhibitors, aprotinin and urinary trypsin inhibitor (UTI), on the cute pancreatitis, this study was carried out in dogs of acute pancreatitis induced by oleic acid (0.28 mg/kg). Administration with aprotinin and UTI seemed to have a therapeutic effect on the clinical sign, ultrasonographic finding, histopathologic finding. But in amylase and lipase activity, there were no significant differences among three groups.

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Isolation of endonuclease inhibitor from tobacco chloroplaut (담배 엽록체에서 제한효소 저해물의 분리)

  • 조영동;심성태
    • Journal of the Korean Society of Tobacco Science
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    • v.10 no.1
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    • pp.37-47
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    • 1988
  • Endonuclease inhibitor was isolated from the chloroplast of the leaves of tobacco, Burley 21 and NC 83, The inhibitory effect on the activities of endonucleases including BamH1 was lost by the addition of trypsin or heat treatment However, the treatment of $\alpha$-amylase was unconcerned in the inhibitory effect The endonuclease inhibitor was found to be a monomeric protein that plays a vital role for protection of tobacco chloroplast DNA from endonuclease action.

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Genetic Polvmorphism of Protease Inhibitor (Pl) in Korean Population (한국인 집단에서 Protease inhibitor(PI)의 유전적 다형)

  • 김현섭;강신성
    • The Korean Journal of Zoology
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    • v.38 no.2
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    • pp.294-298
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    • 1995
  • The genetic polymorphism of Protease inhibitor (Pl) in Korean population was investigated by using isoelectric focusing (IEF) in an ultra-narrow pH range,4.2-4.9, and immunoblottins. Three common alleles (Pl * Ml, Pl*2, Pl * M3) were observed and the frequencies for the alleles were Pl * M1=0.7843, Pl * M2=0.1613, Pl * M3=0.0323. In addition to the three common alleles, rare alleles (Pl *5, Pl * Z, Pl* H were detected at low-level frequency. Two unknovlm variants, which were not reported on previous studies in Korean population, were also found.

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A Cholesterol Biosynthesis Inhibitor from Rhizopus oryzae

  • Kim, Hyun-Jung;Yim, Soon-Ho;Lee, Ik-Soo
    • Archives of Pharmacal Research
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    • v.27 no.6
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    • pp.624-627
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    • 2004
  • A bile acid derivative, methyl chalate (1), was isolated from EtOAc extract of the fungus Rhizopus oryzae as a cholesterol biosynthesis inhibitor. It showed moderate inhibitory activity on cholesterol biosynthesis in human Chang liver cells. Compound 1 exhibited inhibitory effect on the later step of cholesterol biosynthesis, indicating that its action mode is different from that of statins that act on the HMG-CoA reductase.