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| 1.
論文 |
論文
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Matsuo, Jun-ichi ; Okuno, Ryosuke ; Takeuchi, Kosuke ; Kawano, Mizuki ; Ishibashi, Hiroyuki
概要:
金沢大学医薬保健研究域薬学系<br />Optimized reaction conditions for the preparation of various 2-monosubstituted 3-ethoxycyclobutanone
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s are described. 2-Monoalkyl 3-ethoxycyclobutanones were efficiently prepared by the reaction of the corresponding carboxylic acid chlorides and an excess amount of ethyl vinyl ether in the presence of diisopropylethylamine at 90 °C in a sealed tube. 2-Monoaryl 3-ethoxycyclobutanones were prepared by using 2,6-lutidine as a base in the above-mentioned procedure. © 2010 Published by Elsevier Ltd. All rights reserved.
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| 2.
論文 |
論文
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Matsuo, Junichi ; Okuno, Ryosuke ; Takeuchi, Kosuke ; Kawano, Mizuki ; Ishibashi, Hiroyuki
概要:
金沢大学医薬保健研究域薬学系<br />Optimized reaction conditions for the preparation of various 2-monosubstituted 3-ethoxycyclobutanone
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s are described. 2-Monoalkyl 3-ethoxycyclobutanones were efficiently prepared by the reaction of the corresponding carboxylic acid chlorides and an excess amount of ethyl vinyl ether in the presence of diisopropylethylamine at 90 °C in a sealed tube. 2-Monoaryl 3-ethoxycyclobutanones were prepared by using 2,6-lutidine as a base in the above-mentioned procedure. © 2010 Elsevier Ltd. All rights reserved.
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| 3.
図書 |
図書
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Nagarjuna ; aus dem chinesischen Text des Kumarajiva übersetzt und mit einem Kommentar herausgegeben von Lutz Geldsetzer
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| 5.
論文 |
論文
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Yamaguchi, Junpei ; Sasaki, Motoko ; Sato, Yasunori ; Itatsu, Keita ; Harada, Kenichi ; Zen, Yoh ; Ikeda, Hiroko ; Nimura, Yuji ; Nagino, Masato ; Nakanuma, Yasuni
概要:
医薬保健研究域医学系<br />Polycomb group protein EZH2, frequently overexpressed in malignant tumors, is the catalytic subunit of p
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olycomb repressive complex 2 (PRC2). PRC2 interacts with HDACs in transcriptional silencing and relates to tumor suppressor loss. We examined the expression of HDAC isoforms (HDAC 1 and 2) and EZH2, and evaluated the possible use of HDAC inhibitor suberoylanilide hydroxamic acid (SAHA) and EZH2 repressor for gallbladder carcinoma. We used 48 surgically resected gallbladders and cultures of human gallbladder epithelial cells (HGECs), gallbladder carcinoma (TGBC2TKB), and cholangiocarcinoma (HuCCT-1 and TFK-1) cell lines for examination. Immunohistochemically, EZH2 was overexpressed in gallbladder carcinoma, especially poorly differentiated carcinoma, but not in normal epithelium. In contrast, HDAC1/2 were expressed in both carcinoma and normal epithelium in vivo. This pattern was verified in cultured cells; EZH2 was highly expressed only in TGBC2TKB, whereas HDAC1/2 were expressed in HGECs and TGBC2TKB. Interestingly, SAHA treatment caused significant cell number decline in three carcinoma cells, and this effect was synergized with EZH2 siRNA treatment; however, HGECs were resistant to SAHA. In TGBC2TKB cells, the expression of EZH2 and HDAC1/2 were decreased by SAHA treatment, and p16INK4a, E-cadherin, and p21were simultaneously activated; however, no such findings were obtained in HGECs, suggesting that the effect of SAHA depends on the EZH2-mediated tumor suppressor loss. In conclusion, this study suggests a possible mechanism by which carcinoma cells but not normal cells are sensitive to SAHA and indicates the efficacy of this new anticancer agent in combination with EZH2 repression in gallbladder carcinoma. © 2009 Japanese Cancer Association.
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| 6.
論文 |
論文
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Fukuyoshi, Shuichi ; Ooi, Takashi ; Nakagaki, Ryoichi
概要:
The crystal structure of 2-[1-(2,4-dinitrophenyl)ethyl]-1,10-phenanthroline was determined by X-ray crystallography. The
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compound crystallizes in a monoclinic system and was characterized thus: P21/n, a = 15.477(2), b = 5.1818(6), c = 21.754(2)Å, β = 96.295(3)°, Z = 4, V = 1734.12 Å3. The crystal structure was solved by direct methods and refined by full-matrix least-squares on F2 to final values of R = 0.0600.
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| 7.
論文 |
論文
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Sato, Hiroshi ; Takino, Takahisa
概要:
Membrane-type matrix metalloproteinase-1 (MT1-MMP) mediates cleavage of not only MMP-2/gelatinase A for activation, but
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also a variety of substrates including type I collagen (reviewed in Cancer Sci 2005; 96: 212-7). MMP-2 activation involves tissue inhibitor of MMP (TIMP)-2 as a bridging molecule between MT1-MMP and pro-MMP-2. Thus, net activity of MT1-MMP and MMP-2 is regulated in a complex manner depending on TIMP-2 concentration. During invasive growth of tumor cells in type I collagen matrix, MT1-MMP initiates denaturation of collagen into gelatin, which is subsequently digested further by MMP-2 adjacent to MT1-MMP. Coordinate action of MT1-MMP and MMP-2 may facilitate pericellular proteolysis, and enhance not only tumor invasion/migration but also cell growth. Tetraspanins as binding proteins of MT1-MMP regulate MT1-MMP subcellular localization and compartmentalization, leading to efficient MMP-2 activation and proteolysis coupled with cellular function. © 2010 Japanese Cancer Association.
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| 8.
論文 |
論文
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Sakata, Ryo ; Iwamoto, Ryoji ; Fujinami, Shuhei ; Ukaji, Yutaka ; Inomata, Katsuhiko
概要:
金沢大学理工研究域物質化学系<br />t-Butyl 3,4-dialkyl-1H-pyrrole-2-carboxylates were oxidized with ochloranil in the presence of MeOH
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to afford the corresponding 5-methoxypyrrolin-2-one derivatives. The resulting 5-methoxypyrrolin-2-one was reacted with various nucleophiles under acidic conditions to afford the functionalized pyrrolinone derivatives in good yields. © The Japan Institute of Heterocyclic Chemistry.
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| 9.
論文 |
論文
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Mohri, Takuya ; Nakajima, Miki ; Fukami, Tatsuki ; Takamiya, Masataka ; Aoki, Yasuhiro ; Yokoi, Tsuyoshi
概要:
金沢大学医薬保健研究域薬学系<br />Human CYP2E1 is one of the pharmacologically and toxicologically important cytochrome P450 isoforms.
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Earlier studies have reported that the CYP2E1 expression is extensively regulated by post-transcriptional and post-translational mechanisms, but the molecular basis remains unclear. In the present study, we examined the possibility that microRNA may be involved in the post-transcriptional regulation of human CYP2E1. In silico analysis identified a potential recognition element of miR-378 (MRE378) in the 3'-untranslated region (UTR) of human CYP2E1 mRNA. Luciferase assays using HEK293 cells revealed that the reporter activity of the plasmid containing the MRE378 was decreased by co-transfection of precursor miR-378, indicating that miR-378 functionally recognized the MRE378. We established two HEK293 cell lines stably expressing human CYP2E1 including or excluding 3'-UTR. When the precursor miR-378 was transfected into the cells expressing human CYP2E1 including 3'-UTR, the CYP2E1 protein level and chlorzoxazone 6-hydroxylase activity were significantly decreased, but were not in the cells expressing CYP2E1 excluding 3'-UTR. In both cell lines, the CYP2E1 mRNA levels were decreased by overexpression of miR-378, but miR-378 did not affect the stability of CYP2E1 mRNA. In a panel of 25 human livers, no positive correlation was observed between the CYP2E1 protein and CYP2E1 mRNA levels, supporting the post-transcriptional regulation. Interestingly, the miR-378 levels were inversely correlated with the CYP2E1 protein levels and the translational efficiency of CYP2E1. In conclusion, we found that human CYP2E1 expression is regulated by miR-378, mainly via translational repression. This study could provide new insight into the unsolved mechanism of the post-transcriptional regulation of CYP2E1. Copyright 2009 Elsevier Inc. All rights reserved.
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電子ブック |
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