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11.
Dr. Daisuke Okuno Dr. Noriho Sakamoto Dr. Mohammed S. O. Tagod Yoshiko Akiyama Dr. Sakiko Moriyama Dr. Takuto Miyamura Dr. Atsuko Hara Dr. Takashi Kido Dr. Hiroshi Ishimoto Prof. Yuji Ishimatsu Prof. Takashi Tanaka Prof. Jun Ishihara Prof. Kohsuke Takeda Prof. Yoshimasa Tanaka Prof. Hiroshi Mukae 《ChemMedChem》2021,16(16):2515-2523
Heat shock protein 47 (HSP47), a collagen-specific molecular chaperone, is causally related to fibrotic diseases, including idiopathic pulmonary fibrosis. The identification of Compounds that interfere with the HSP47-collagen interaction is essential for the development of relevant therapeutics. Herein, we prepared human HSP47 as a soluble fusion protein expressed in E. coli and established an assay system for HSP47 inhibitor screening. We screened a natural and synthetic Compound library established at Nagasaki University. Among 1023 Compounds, 13 exhibited inhibitory activity against human HSP47, of which three inhibited its function in a dose-dependent manner. Epigallocatechin-3-O-gallate, one of these three Compounds, is a typical polyphenol Compound derived from tea leaves. Structurally related Compounds were synthesized and examined for their activity, revealing a hydroxyl group at A-ring position 5 as important for its activity. The present findings provide valuable insight for the development of natural product-derived therapeutics for fibrotic diseases, including idiopathic pulmonary fibrosis. 相似文献
12.
Dr. Daisuke Fujiwara Kousuke Mihara Ryo Takayama Yusuke Nakamura Prof. Mitsuhiro Ueda Prof. Takeshi Tsumuraya Prof. Ikuo Fujii 《Chembiochem : a European journal of chemical biology》2021,22(24):3406-3409
Conformationally constrained peptides hold promise as molecular tools in chemical biology and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chemically modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip - 3 retained the α-helical structure and bound to AurA with a KD value of 13.7 μM. Bip - 3 and the adenosine-tethered peptide Bip - 3 - Adc provided IC50 values of 103 μM and 7.7 μM, respectively, suggesting that Bip - 3 - Adc bivalently inhibited AurA. In addition, the selectivity of Bip - 3 - Adc to several protein kinases was tested, and was highest against AurA. These results demonstrate that chemical modification can enable the construction of a kinase-focused library of phage-displayed HLH peptides. 相似文献
13.
Toshihide Suzuki Teruo Miyazawa Kenshiro Fujimoto Miki Otsuka Masako Tsutsumi 《Lipids》1993,28(8):775-778
The levels of phosphatidylcholine hydroperoxide in serially cultured human fetal diploid fibroblasts at various population
doubling levels were determined by high-performance liquid chromatography combined with chemiluminescence detections. This
methodology utilizes a mixture of cytochromec and luminol as post-column hydroperoxide group specific luminescent reagents. The cellular hydroperoxide content increased
with age from 0.34 to 27.72 pmol/106 cells. At the end of the cells'in vitro lifespan (51st population doubling level), the hydroperoxide content per 106 cells reached about 80 times the level found in cells of the 20th population doubling level. Supplementation of exogenous
α-tocopherol to the culture medium prevented hydroperoxide accumulation, but did not extent the lifespanin vitro. The results indicate that substantial intracellular phospholipid hydroperoxide accumulation occurred in the course of aging
of human fetal liploid fibroblasts. 相似文献
14.
Crosslinked poly(N-benzyl-4-vinyipyridinium bromide) has been found to be digested by activated sludge obtained from sewage works. As an extension of this work, the authors attempted to make poly(methyl methacrylate) biodegradable by incorporation of a pyridinium group. Poly(methyl methacrylate) containing a small amount of N-benzyl-4-vinylpyridinium chloride in the main chain showed remarkable reduction in molecular weight and gravimetric weight when placed in an aeration tank of a sewage works. Molecular weight reduction by activated sludge was more conspicuous when content of the pyridinium group was larger and the original molecular weight before the biological treatment was lower. Since insoluble pyridinium-type polymer captures microbial cells alive, this biodegradation appears to be facilitated by enhancement of affinity of the synthetic hydrophobic polymer with cells of microogranisms. © 1994 John Wiley & Sons, Inc. 相似文献
15.
Atsuhiko Yamanaka Tooru Kitagawa Masayuki Tsutsumi Toshihiro Kashima Hiroyuki Fujishiro Kimiko Ema Yoshinobu Izumi Shigehiro Nishijima 《应用聚合物科学杂志》2004,93(6):2918-2925
High strength polyethylene fiber (Toyobo, Dyneema® fiber: hereinafter abbreviated to DF) has a negative thermal expansion coefficient. Relation between fiber structure and thermal strain of DF used as reinforcement of DF reinforced plastic (DFRP) for cryogenic use was investigated. The crystallinities and orientation angles of several kinds of polyethylene fibers having different modulus from 15 to 134Gpa (herein after abbreviated to DFs) were measured by NMR and X‐ray. We obtained the parameters of the mechanical series‐parallel model composed of crystal and amorphous by crystallinity and modulus. Thermal expansion coefficients of DFs were estimated by mechanical series‐parallel model. All DFs having different modulus showed negative thermal expansion coefficients in the temperature range from 180 to 300K, and absolute values of those markedly increased by increasing tensile modulus of DF. The estimated thermal expansion coefficients showed negative values, and thermal strains showed a similar curve to observed ones mostly. Average thermal expansion coefficients in the temperature range from 180 to 300K estimated by mechanical model agreed with the observed ones. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 93: 2918–2925, 2004 相似文献
16.
Y. Tsutsumi 《Powder Technology》1973,7(3):181-188
The volume of the unit cell of a powder bed in a general case is calculated, and an equation is proposed for calculating the porosity of the bed consisting of uniformly sized ellipsoidal particles in contact and regularly arranged. In the case of uniformly sized spherical particles in contact, the equation can be simplified.Three dimensions and face angles of the unit cell are given for each regular arrangement both in cases of ellipsoidal and spherical particles. The values of the porosity are calculated by using the author's equation: the results for both ellipsoids and spheres are equal when tire particle arrangements are the same.The face angles of the unit cells proposed by Graton and Fraser are modified in two cases by the author's method of calculation and a system omitted from their classification is described. Other equations for calculation of the porosity are discussed. 相似文献
17.
Toshihiro Nagao Yuji Shimada Yoshie Yamauchi-Sato Takaya Yamamoto Masaaki Kasai Kentaro Tsutsumi Akio Sugihara Yoshio Tominaga 《Journal of the American Oil Chemists' Society》2002,79(3):303-308
A commercial product of CLA contains almost equal amounts of cis-9,trans-11 (c9,t11)-CLA and trans-10,cis-12 (t10,c12)-CLA. We attempted to enrich the two isomers by a two-step selective esterification using Candida rugosa lipase that acted on c9,t11-CLA more strongly than on t10,c12-CLA. An FFA mixture containing CLA isomers was esterified with an equimolar amount of lauryl alcohol in a mixture of 20%
water and the lipase. When the esterification of total FA reached 50%, two isomers were fractionated in a good yield: t10,c12-CLA was enriched in FFA, and c9,t11-CLA was recovered in lauryl esters. The FFA were esterified again to enrich t10,c12-CLA. At 27.3% esterification of total FA, the t10,c12-CLA content in FFA increased to 64.8 wt% with 89.3% recovery: The ratio of the content of t10,c12-CLA to that of two isomers was 95.9%. Lauryl esters obtained by the single esterification were employed for enrichment
of c9,t11-CLA. After the esters were hydrolyzed, the resulting FFA were esterified again with lauryl alcohol. At 62.0% esterification
of total FA, the c9,t11-CLA content in lauryl esters increased to 73.3 wt% with 79.4% recovery: The ratio of the content of c9,t11-CLA to that of two isomers was 95.6%. In a 600-g-scale purification, molecular distillation was effective in separating
the reaction mixture into lauryl alcohol, FFA, and lauryl ester fractions. 相似文献
18.
Riho Kataishi Takayuki Ikeda Toshiki Sasaki Kouhei Toyotaka Daiki Nakamura Hiroyuki Miyake Yuji Iwaki Kazunori Watanabe Yuichi Yanagisawa Hisao Ikeda Harue Nakashima Nobuharu Ohsawa Shingo Eguchi Satoshi Seo Yoshiharu Hirakata Shunpei Yamazaki Daisuke Kurosaki Masakatsu Ohno Chris Bower Darryl Cotton Andrew Matthews Piers Andrew Catalin Gheorghiu Johan Bergquist 《Journal of the Society for Information Display》2014,22(8):381-392
In this study, white organic electroluminescent devices with microcavity structures were developed. A flexible high‐resolution active‐matrix organic light‐emitting diode display with low power consumption using red, green, blue, and white sub‐pixels formed by a color‐filter method was fabricated. In addition, a side‐roll touch display was developed in combination with a capacitive flexible touch screen. 相似文献
19.
Katsuhiro Inomata Daisuke NakanishiAi Banno Eiji NakanishiYosuke Abe Ryuta KuriharaKentaro Fujimoto Takuhei Nose 《Polymer》2003,44(18):5303-5310
Association behavior and physical gelation mechanism of ABA triblock copolymer dissolved in B-selective solvent have been studied systematically from dilute to moderately concentrated solutions. Static and dynamic light scattering and nuclear magnetic resonance measurements for dilute solutions of poly(methyl methacrylate)-block-poly(tert-butyl acrylate)-block-poly(methyl methacrylate) (PMMA-PtBuA-PMMA) in 1-butanol (PtBuA selective solvent) indicated that PMMA-PtBuA-PMMA chains are molecularly dissolved above 50 °C. With decreasing temperature, the triblock copolymers form associated micelles consisting PMMA associated core and PtBuA shell. Linear dynamic viscoelastic measurements for solutions with moderate concentration (3.9-12.0 wt%) revealed that the system was viscous sol state at 60 °C. Drastic increase of shear storage modulus (G′) occurred with decreasing temperature, and at 25 °C, G′ showed rubbery plateau with weak frequency dependency, means the formation of elastic physical gel. The consistency between the temperature for micelle formation and that at the increase in G′ indicates that the physical gelation is owing to the network formation as the result of the association of PMMA chains and the bridging PtBuA chains connecting the PMMA cores. Master curves for the dynamic moduli were derived by time-temperature superposition along the frequency axis. Just above sol-gel transition concentration (Cgel), the master curves suggest the existence of fairy amount of aggregate that is not incorporated in the macroscopic network. With the increase in polymer concentration, the master curves become to reveal Maxwell-type viscoelasticity with narrow relaxation time distribution, suggesting the formation of transient network with easily generation and destruction of crosslinks. Concentration dependency of the plateau modulus is stronger than the theoretically expected, means the macroscopic transient network grows with polymer concentration by increasing the fraction of elastically effective bridging PtBuA chain above Cgel. 相似文献
20.
1 INTRODUCTION Since Cu-ZSM-5 was reported as an effective catalyst for the selective catalytic reduction (SCR) of NO by hydrocarbons in the presence of excess oxygen, the SCR of NOx has received much attention as a kind of potential technology for cleaning NOx in various oxygen-rich exhausts of diesel engine, lean burning gasoline engine and gas engine. Although a number of catalysts have been tested, to date, it still seems to be difficult to find a catalyst that is completely suit… 相似文献