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121.
Keisuke Maruyama Masaharu Nakamura Shusuke Tomoshige Kazuyuki Sugita Makoto Makishima Yuichi Hashimoto Minoru Ishikawa 《Bioorganic & medicinal chemistry letters》2013,23(14):4031-4036
Our multi-template approach for drug discovery, focusing on protein targets with similar fold structures, has yielded lead compounds for various targets. We have also shown that a diphenylmethane skeleton can serve as a surrogate for a steroid skeleton. Here, on the basis of those ideas, we hypothesized that the diphenylmethane derivative bisphenol A (BPA) would bind to the ligand-binding domain of estrogen receptors (ERs) in a similar manner to estradiol and act as a steroid surrogate. To test this idea, we synthesized a series of BPA analogs and evaluated their structure-activity relationships, focusing on agonistic/antagonistic activities at ERs and ERα/ERβ subtype selectivity. Among the compounds examined, 18 was found to be a potent ERα-antagonist with high selectivity over ERβ and androgen receptor under our assay conditions. A computational docking study suggested that 18 would bind to the antagonistic conformation of ERα. ERα-selective antagonists, such as 18, are candidate agents for treatment of breast cancer. 相似文献
122.
Toshiko Kido Katsuyuki Tanizawa Kenji Inagaki Tohru Yoshimura Masaaki Ishida Katsumi Hashizume 《Bioscience, biotechnology, and biochemistry》2013,77(10):2549-2554
2-Nitropropane dioxygenase, purified to homogeneity by an improved method from a yeast, Hansenula mrakii, has a molecular weight of 42,000, and consists of a single polypeptide. The enzyme contains 1 mol of FAD per mol of enzyme. The iron protein associated with previous preparations was removed by the present purification procedures. The enzyme catalyzes the oxygenative denitrification of anionic nitroalkanes much more effectively than that of the neutral ones with the optimum pH of 6.5. The Michaelis constants for the anionic substrates are as follows: 2-nitropropane, 1.61 mM; 1-nitropropane, 3.23 mM; nitroethane, 3.13 mM, and 3-nitro-2-butanol, 0.59 mM. 相似文献
123.
Norio Kurihara Yuzuru Sanemitsu Tomio Kimura Masaharu Kobayashi Minoru Nakajima Yoshiyuki Tamura 《Bioscience, biotechnology, and biochemistry》2013,77(5):784-797
β-BTC(3, 4/5, 6),1) γ-BTC(3, 4, 6/5), and ε-BTC(3, 4, 5/6) were synthesized from α-BTC (3, 6/4, 5) by stepwise routes. 相似文献
124.
Osamu Yamada Akira Kurozumi Fumio Futatsuya Kensaku Ito Shuichi Ishida Katsura Munakata 《Bioscience, biotechnology, and biochemistry》2013,77(7):1467-1471
Some benzophenones substituted with methyl, methoxy, hydroxy or halogen groups inhibited growth and induced chlorosis in various plants. The structure activity relationships about the chlorosis-inducing activity and the growth inhibitory activity of the 3-methyl-benzophenones were well expressed by use of hydrophobic contant π, and Hammett’s σ. The highest selectivity for phytotoxic activities against barnyardgrass and the rice plant was with 3,3′-dimethyl-4-methoxybenzophenone (Methoxyphenone). 相似文献
125.
Kazuaki Manabe Mitsuyoshi Morii Masaru Honjo Masaharu Ohoka Kouichiro Fushimi Akiko Sawakura 《Bioscience, biotechnology, and biochemistry》2013,77(8):2261-2267
Bacillus subtilis 1A20 transformed with a hybrid plasmid, pNP150, to which a DNA fragment from Bacillus amyloliquefaciens F was attached, produced a large amount of a neutral protease. To identify the origin of the gene specifying this neutral protease, neutral proteases from B. amyloliquefaciens F, B. subtilis NP58 (a derivative of Marburg 6160), and B. subtilis 1A20 transformed with pNP150 were purified. We investigated their immunological properties and primary structures.The proteases from these two species were indistinguishable by chromatography, but they were distinguishable from each other by SDS-polyacrylamide gel electrophoresis and double immunodiffusion. Amino acid sequencing of these two proteases by Edman degradation showed that there were four substitutions in the 20-residue amino acid sequence from the N-termini.Neutral protease from the transformant had the same immunological characteristics and N-terminal amino acid sequence as that from B. amyloliquefaciens. These results meant that the gene in question was derived from a gene specifying the neutral protease in this bacterium. 相似文献
126.
Oxalacetate carboxylyase was extracted from pig heart muscle and purified about 40 fold by means of acid and heat treatments, salting out and three steps of column chromatography. Some properties of the enzyme were studied by manometric and spectrophotometric measurements. The enzyme activity was optimal at pH 7. Km for oxalacetate was 4.3 × 10?3 m/liter and the activation energy of the enzyme reaction was 15 kcal/m. The enzyme was activated by certain bivalent cations, among which Mn2+ was the most effective. Cu2+, Hg2+, some metal chelating reagents (EDTA, citrate and Oxalate) and pCMB strongly inhibited the enzyme activity. Inhibition by avidin was not observed, suggesting that biotin was not involved in the reaction as the prosthetic group of the enzyme. 相似文献
127.
Shuichi Ishida Mitsuo Ida Osamu Yamada 《Bioscience, biotechnology, and biochemistry》2013,77(4):410-421
Formation of a sulfonium-like intermediate was assumed in the hydrolysis of the 2-bromoethylthiobenzenes. A linear free energy relationship was found between the hydrolysis rate of a certain substituted 2-bromoethylthiobenzene and the molar fraction of water in the solvent. The effect of the substituent on the rate constant was attributed not only to the activation energy but also to the entropy change of activation. The negative ρ-value in the formation of the sulfonium-like intermediate in aqueous solution was comparable with that obtained in the ρ-σ-π analysis for ovicidal activity of the compounds.For the reaction of the substituted 2-bromoethylthiobenzenes with highly excess amount of 4-(p-nitrobenzyl)-pyridine, the ρ-value was found to be negative, which means that the formation of the sulfonium-like intermediate is a rate determining step. Whichever might be more important, the hydrolysis or alkylation, as to the ovicidal action of the compounds, the formation of the sulfonium-like intermediate, could be considered to be an essential step. 相似文献
128.
Kouta Takeda Takuya Ishida Kiyohiko Igarashi Masahiro Samejima Hiroyuki Ohno 《Bioscience, biotechnology, and biochemistry》2013,77(7):1195-1198
Pyrroloquinoline quinone-dependent quinoprotein alcohol dehydrogenases (PQQ-ADH) require ammonia or primary amines as activators in in vitro assays with artificial electron acceptors. We found that PQQ-ADH from Pseudomonas putida KT2440 (PpADH) was activated by various primary amines, di-methylamine, and tri-methylamine. The alcohol oxidation activity of PpADH was strongly enhanced and the affinity for substrates was also improved by pentylamine as an activator. 相似文献
129.
Osamu Yamada Shuichi Ishida Fumio Futatsuya Kensaku Ito Hiroshi Yamamoto Katsura Munakata 《Bioscience, biotechnology, and biochemistry》2013,77(6):1235-1240
The discovery that anisomycin showed plant growth-regulating activity led to the investigation of compounds having p-methoxyphenyl group; the p-anisole derivatives. 4-Methoxydiphenylmethanes and related compounds inhibited the growth of both shoots and roots in test plants. Growth-inhibitory activity in the series of 4-methoxydiphenylmethanes was lowered by an increase in the electron donating or withdrawing ability of the substituent and was parabolically dependent on the Hammett’s σ. Selective actions of these compounds in their growth inhibition are discussed based on correlations between their activities against barnyard grass and other test plants.Some 4-methoxydiphenylmethanes induced chlorosis, a disturbance in phototropism or geotropism, and root hypertrophy. 相似文献
130.
Masahiko Ishida Hideo Nagayama Kensuke Shimura 《Bioscience, biotechnology, and biochemistry》2013,77(8):1881-1892
The biosynthetic pathway of vitamin B6 (abbreviated as Be) has been studied with the cell-suspension of B6-producing bacteria, Achromobacter cycloclastes A.M.S. 6201. The distribution of 14C in the Be molecule prepared with the cell-suspensions containing glycerol-1,3-14C, glycerol-2-14C or γ-aminobutyric acid-U-14C was investigated by using three novel degradation methods. The results showed that carbon skeletons of glycerol and γ-aminobutyric acid were used for the formation of the major part of B6 carbon skeleton respectively. The implication of these compounds as precursors of B6 was discussed. 相似文献