• Genomics & Informatics
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• 제18권4호
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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.

• Journal of Microbiology and Biotechnology
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• 제20권11호
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• pp.1521-1523
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• 2010

Bioassay-guided fractionation of a methanol extract of Ganoderma lucidum gave a pure cholesterol esterase inhibitor. On the basis of spectroscopic analysis and comparison with data from the literature, the structure of this compound was identified as $5{\alpha},8{\alpha}$-epidioxyergosta-6,22-dien-$3{\bet}$-ol (compound I). This compound inhibited cholesterol esterase activity with an $IC_{50}$ value of $42{\mu}M$. Lineweaver-Burk plot analysis revealed that compound I is a noncompetitive inhibitor. The findings of this study suggest that compound I may be the active principle of the hypocholesterolemic effect of Ganoderma lucidum.

• BMB Reports
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• 제50권12호
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• pp.640-646
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• 2017

Regulatory B cells, also well-known as IL-10-producing B cells, play a role in the suppression of inflammatory responses. However, the epigenetic modulation of regulatory B cells is largely unknown. Recent studies showed that the bromodomain and extra-terminal domain (BET) protein inhibitor JQ1 controls the expression of various genes involving cell proliferation and cell cycle. However, the role of BET proteins on development of regulatory B cells is not reported. In this study, JQ1 potently suppressed IL-10 expression and secretion in murine splenic and peritoneal B cells. While bromodomain-containing protein 4 (BRD4) was associated with $NF-{\kappa}B$ on IL-10 promoter region by LPS stimulation, JQ1 interfered the interaction of BRD4 with $NF-{\kappa}B$ on IL-10 promoter. In summary, BRD4 is essential for toll like receptor 4 (TLR4)-mediated IL-10 expression, suggesting JQ1 could be a potential candidate in regulating IL-10-producing regulatory B cells in cancer.

• E2M - 전기 전자와 첨단 소재
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• 제9권1호
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• pp.38-43
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• 1996

A coprecipitation method was used for preparing Ca and Pt doped $SnO_2$ fine powder. Components of the powder were investigated by XPS and SIMS. Crystallite size and specific surface area were investigated by TEM, XRD, and BET analysis. $SnO_2$(Ca)/Pt based thick film devices were prepared by a screen printing technique for methane gas detection. Then sensing characteristics of the devices were investigated. As Ca and Pt added, the crystal growth of $SnO_2$ was suppressed during calcining and sintering, and the sensitivity of $SnO_2$(Ca)/Pt thick film to methane gas was enhanced. For the Pt doped $SnO_2$ fine particle, the thick film device shows sensitivity of about 83% to 2000 ppm methane gas at an operating temperature of >$400^{\circ}C$.

• Applied Biological Chemistry
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• 제48권3호
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• pp.189-200
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• 2005

생물학적 질소고정과정의 연구는 학문적으로나 산업적으로 매우 중요한 과정이다. 본 총설에서는 공업적 질소고정과 비교되는 생물학적 질소고정의 특징을 간단히 살펴보고, Azotobacter vinelandii에서 연구되고 있는 생물학적 질소고정효소의 특징을 다룬다. 생물학적 질소고정과정은 다양한 생명체에서 일어나며, 최근에는 미생물인 A. vinelandii에 그 작용 메커니즘에 관한 연구가 집중되어 있다. 공기중의 질소를 암모니아로 변환시키는 질소고정은 화학적으로 환원 반응에 해당하므로 전자의 공급이 필요하다. 생물학적 질소고정을 담당하는 질소고정효소는 촉매반응을 위해 생물학적인 환원력을 사용하여 전자를 공급받아, Fe 단백질의 $Fe_4S_4$ cluster와 MoFe 단백질의 P-cluster를 거쳐 질소 환원 반응이 일어나는 FeMo-cofactor로 전달한다. 이러한 전자전달의 과정과 수소이온의 전달 과정은 질소고정효소의 반응 메커니즘 이해에 매우 중요한 과정이며, FeMo-cofactor와 질소분자의 상호작용은 생물학적 질소고정 메커니즘의 중심에 있다. 질소고정 작용 메커니즘의 연구에는 X-선 단백질 결정학, EPR과 $M{\ddot{u}}ssbauer$ 등의 다양한 분광학적 방법과, 효소의 기질과 저해제의 상호작용을 연구하고 mutant와 비교하는 생화학적 접근방법, 그리고 FeMo-cofactor의 모델 화합물을 합성하여 연구하는 화학적 방법 등이 적용되었다. 이들 분야의 최근 연구결과를 소개하며, 마지막으로, 다양한 연구 결과에 바탕하여 새로운 질소고정효소의 작용 기작이 제안하였다.