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123.
Kaya T Nagamine K Matsui N Yasukawa T Shiku H Matsue T 《Chemical communications (Cambridge, England)》2004,(2):248-249
[small beta]-Galactosidase expression in a small number of Escherichia coli cells has been measured in real time with an electrochemical sensor chip. E. coli cells were embedded using collagen gel within a micropore which was microfabricated onto a chip. The activity of the expressed [small beta]-galactosidase was determined using p-aminophenyl [small beta]-d-galactopyranoside (PAPG) as a substrate. 相似文献
124.
[structure: see text] Polyenyne macrocycles with pi-extended [9]- and [12]radialene frameworks have been synthesized. These radialenes exhibit restricted rotation of the aromatic rings, and the D3- and D4-symmetric structures in solutions have been determined by dynamic NMR. The macrocyclic radialenes bear small to medium inner cavities, and the small cavity of the pi-extended [9]radialene can incorporate a silver cation. 相似文献
125.
Nishida H Miyazaki Y Mukaihira T Saitoh F Fukui M Harada K Itoh M Muraoka A Matsusue T Okamoto A Hosaka Y Matsumoto M Ohnishi S Mochizuki H 《Chemical & pharmaceutical bulletin》2002,50(9):1187-1194
Intravascular clot formation is an important event in a number of cardiovascular diseases. The prevention of blood coagulation has become a major target for new therapeutic agents. Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in the blood coagulation cascade and represents an attractive target for anticoagulant drug development. We have investigated substituents in the central part of a lead compound (3: M55113), and discovered that compound M55551 (34: (R)-4-[(6-Chloro-2-naphthalenyl)sulfonyl]-6-oxo-1-[[1-(4-pyridinyl)-4-piperidinyl]methyl]-2-piperazinecarboxylic acid) is a potent inhibitor of FXa (IC(50)=0.006 microM), with high selectivity for FXa over trypsin and thrombin. The activity of this compound is ten times more powerful than the lead compound. 相似文献
126.
Dr. Hiroshi Hinou Risho Miyoshi Yasuaki Takasu Hirokazu Kai Dr. Masaki Kurogochi Dr. Shingo Arioka Dr. Xiao‐Dong Gao Dr. Nobuaki Miura Dr. Naoki Fujitani Dr. Shinya Omoto Dr. Tomokazu Yoshinaga Dr. Tamio Fujiwara Dr. Takeshi Noshi Dr. Hiroko Togame Prof. Hiroshi Takemoto Prof. Shin‐Ichiro Nishimura 《化学:亚洲杂志》2011,6(4):1048-1056
A potent inhibitor for Vibrio cholerae neuraminidase (VCNA) was developed by using a novel two‐step strategy, a target amino acid validation using mechanism‐based labeling information, and a potent inhibitor search using a focused library. The labeling information suggested the hidden dynamics of a loop structure of VCNA, which can be a potential target of the novel inhibitor. A focused library composed of 187 compounds was prepared from a 9‐azide derivative of 2,3‐dehydro‐N‐acetylneuraminic acid (DANA) to interrupt the function of the loop of the labeled residues. Inhibitor 3c showed potent inhibition properties and was the strongest inhibitor with FANA, a N‐trifluoroacetyl derivative of DANA. Validation studies of the inhibitor with a detergent and a Lineweaver–Burk plot suggested that the 9‐substitution group would interact hydrophobically with the target loop moiety, adding a noncompetitive inhibition property to the DANA skeleton. This information enabled us to design compound 4 having the combined structure of 3c and FANA. Compound 4 showed the most potent inhibition (Ki=73 nM , mixed inhibition) of VCNA with high selectivity among the tested viral, bacterial, and mammal neuraminidases. 相似文献
127.
Hiroshi Segawa Tomokazu Iyoda Takeo Shimidzu Kenichi Honda 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(2-3):621-629
The electrochemical and photochemical reduction of the fully methylated derivative of gold meso-tetrakis-(4-pyridyl)porphine (AuTMPyP) in homogeneous solution gives not only a π-radical anion but also its successive product, phlorin, by disproportionation. The electrostatic fixation of AuTMPyP in a Nafion matrix inhibits the latter undesired reaction against effective charge separation, which is explained by the diffusion constant lower by 8 order of magnitude during electrolytic reduction of AuTMPyP compared to that in homogeneous aqueous solution. 相似文献
128.
α, β, γ δ-Tetraphenylporphinatoaluminum carboxylate (TPPA10COR) and phenoxide (TPPA10Ar) bring about the polymerization of β-lactone and epoxide to give polymers with controlled chain length having a carboxylic ester or phenoxy group at the end of each polymer molecule. Acrylate (TPPA10COCH=CH2) and p-vinylphenoxide (TPPA1-OC6H4,CH[dbnd]CH2 (p)) as initiator give polyester or polyether macromer with narrow molecular weight distribution. 相似文献
129.
Yoshiharu Matsumae Yasufumi Takahashi Kosuke Ino Hitoshi Shiku Tomokazu Matsue 《Analytica chimica acta》2014
We evaluated the intracellular NAD(P)H:quinone oxidoreductase (NQO) activity of single HeLa cells by using the menadione–ferrocyanide double-mediator system combined with scanning electrochemical microscopy (SECM). The double-mediator system was used to amplify the current response from the intracellular NQO activity and to reduce menadione-induced cell damage. The electron shuttle between the electrode and menadione was mediated by the ferrocyanide/ferricyanide redox couple. Generation of ferrocyanide was observed immediately after the addition of a lower concentration (10 μM) of menadione. The ferrocyanide generation rate was constant for 120 min. At a higher menadione concentration (100 μM), the ferrocyanide generation rate decreased within 30 min because of the cytotoxic effect of menadione. We also investigated the relationship between intracellular reactive oxygen species or glutathione levels and exposure to different menadione concentrations to determine the optimal condition for SECM with minimal invasiveness. The present study clearly demonstrates that SECM is useful for the analysis of intracellular enzymatic activities in single cells with a double-mediator system. 相似文献
130.
Hayashi H Nihashi W Umeyama T Matano Y Seki S Shimizu Y Imahori H 《Journal of the American Chemical Society》2011,133(28):10736-10739
Liquid crystalline donor (i.e., phthalocyanine) was covalently linked to acceptor (i.e, fullerene) to achieve efficient charge-transport properties in a liquid crystalline phase. The columnar structure exhibited highly efficient ambipolar charge-transport character, demonstrating the potential utility of the strategy in organic electronics. 相似文献