排序方式: 共有16条查询结果,搜索用时 15 毫秒
1.
Fan Zhang Dang Wu Gao-Lei Wang Shuang Hou Ping Ou-Yang Jin Huang Xiao-Yong Xu 《中国化学快报》2017,28(5):1044-1048
A series of novel 1,2,3-benzotriazin-4-one derivatives were designed,synthesized and their inhibitory activities against leulcotriene A_4 hydrolase aminopeptidase in vitro were evaluated.Many compounds showed moderate to good activities at the concentration of 10 μmol/L.Among them,compound Ⅳ-16 exhibited the highest inhibitory activity up to 80.6% with an IC_(50) of 1.30 ± 0.20 μmol/L The compound Ⅳ-16 was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA_4H enzyme by molecular docking was studied.It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study.The relationship between structure and inhibitory activity was also preliminarily discussed. 相似文献
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Marcin Drag Jolanta Grembecka Paweł Kafarski 《Phosphorus, sulfur, and silicon and the related elements》2013,188(6-7):1591-1595
The design, stereo-, and enantioselective synthesis and activity prediction of aminophosphonic acids as new leucine aminopeptidase inhibitors will be discussed. 相似文献
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Stopped-flow radiationless energy transfer experiments have been carried out to investigate the hydrolysis of some dansyl peptide substrates (S) catalyzed by aminopeptidase (E). RET between enzyme tryptophanyl residues and the dansyl group in the substrate allowed direct observation and quantitation of the enzyme-substrate (ES) complexes. Analysis of the stopped-flow RET traces gives kcat = 1.32 s?1 and KM = 47 μM for Leu-Ala-NH(CH2)2NH-Dns (Leu-Ala-DED) and kcat = 4.80 s?1 and KM = 196 μM for Leu-Gly-NH(CH2)2NH-Dns (Leu-Gly-DED). The activation energies of the enzymatic reactions were determined from the Arrhenius plots to be 57 and 38 kJ mol?1 for Leu-Ala-DED and Leu-Gly-DED, respectively. The kinetic results indicate that the enzyme binds Leu-Ala-DED more tightly than Leu-Gly-DED as revealed by a small value of KM. That this enzyme catalyzes the turnover of Leu-Gly-DED more efficiently than Leu-Ala-DED is reflected in a large value of kcat and a small activation energy. The RET signals during the hydrolysis of Leu-Val-NH(CH2)2NH-Dns were extremely weak probably because of the inefficient energy transfer in the ES complex or the retention of the product in the enzyme after completion of the reaction. Aminopeptidase was inactive towards the dansyl compounds of the single amino acid studied. This fact may be due to an unfavorable conformation of these compounds in the ES complexes (small kcat) or a weak binding of the substrates to the enzyme (large KM) or both. 相似文献
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Jolanta Grembecka Artur Mucha Tomasz Cierpicki Paweł Kafarski 《Phosphorus, sulfur, and silicon and the related elements》2013,188(6-7):1739-1743
The structure-based design, synthesis and activity prediction of new leucine aminopeptidase inhibitors, the phosphonamidate and phosphinate dipeptide analogues are presented. 相似文献
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《中国化学快报》2021,32(10):3053-3056
A NIR fluorescent probe (DDAA) derived from fluorophore DDAO with alanine as the recognition group was developed for sensing aminopeptidase N (APN) in gut microbiota. Using DDAA as the real-time guidance tool for the fluorescence imaging of intestinal microorganism, target bacteria and saccharomycete possessing active APN were identified successfully from human feces. 相似文献
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Naminita Gogoi 《Tetrahedron letters》2005,46(44):7581-7582
A total synthesis of the potent aminopeptidase inhibitor (−)-bestatin has been achieved using Shibasaki’s asymmetric Henry reaction catalyzed by an optically active rare earth lanthanum-(R)-binaphthol complex in 26% overall yield. 相似文献
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Rapid screening of aminopeptidase N inhibitors by capillary electrophoresis with electrophoretically mediated microanalysis 下载免费PDF全文
In this work, an electrophoretically mediated microanalysis (EMMA) method with a partial‐filling technique was setup to evaluate the inhibitory potency of novel compounds toward aminopeptidase N (APN). It was necessary to optimize the electrophoretic conditions with respect to the kinetic constraints and for attaining high sensitivity. In our setup, a part of the capillary was filled with the incubation buffer for the enzyme reaction, whereas the rest was filled with a suitable BGE for the separation of substrates and products. To monitor the performance of the newly developed method, the kinetic constants (Km and Vmax) for the catalyzed dissociation of l ‐Leucine‐p‐nitroanilide in the presence of APN as well as the inhibition constant (IC50) of a known competitive inhibitor, that is bestatin, were determined and these results were compared with those obtained by a classical spectrophotometric assay. The developed EMMA method was subsequently applied to the screening of 30 APN inhibitors. Whereas the inhibition potency of these inhibitors (expressed in IC50 values) were significantly underestimated by the EMMA method, the order of the inhibitory potential of these various compounds was found in agreement with the literature. 相似文献
10.
V. K. Jamadar S. N. Jamdar Hari Mohan S. P. Dandekar P. Harikumar 《Radiation Physics and Chemistry》2004,69(6):473-479
Ionizing radiation inactivated purified chicken intestinal aminopeptidase in media saturated with gases in the order N2O>N2>air. The D37 values in the above conditions were 281, 210 and 198 Gy, respectively. OH radical scavengers such as t-butanol and isopropanol effectively nullified the radiation-induced damage in N2O. The radicals (SCN)2•−, Br2•− and I2•− inactivated the enzyme, pointing to the involvement of aromatic amino acids and cysteine in its catalytic activity. The enzyme exhibited fluorescence emission at 340 nm which is characteristic of tryptophan. The radiation-induced loss of activity was accompanied by a decrease in the fluorescence of the enzyme suggesting a predominant influence on tryptophan residues. The enzyme inhibition was associated with a marked increase in the Km and a decrease in the Vmax and kcat values, suggesting an irreversible alteration in the catalytic site. The above observations were confirmed by pulse radiolysis studies. 相似文献