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21.
Protein-ligand interactions may lead to the formation of multiple molecular complexes in dynamic exchange, affecting the kinetic and thermodynamic characteristics of the binding equilibrium. We followed the dissociation kinetics of the transient and specific complex of an antithrombotic peptide N-acetyl-Asp(55)-Phe-Glu-Glu-Ile-Pro(60)-Glu-Glu-Tyr-Leu-Gln(65) with human prothrombin by use of (15)N NMR relaxation dispersion spectroscopy of the peptide. Every one of the five (15)N-labeled adjacent residues of the peptide exhibited apparently different kinetic exchange and relaxation behaviors, which were especially evident at different concentrations of prothrombin. Binding-induced (15)N relaxation dispersion of residues Phe(56), Glu(57), Glu(58), and Ile(59) can be fitted phenomenologically to a two-site on-and-off exchange mechanism with physically feasible relaxation and kinetic parameters obtained for residues Phe(56), Glu(58), and Ile(59), independent of the prothrombin concentration. The apparent kinetic parameters of Glu(57) show some dependence on the concentration of prothrombin and the extracted transverse relaxation rate for Glu(57) in the bound state was severalfold higher than that expected for a protein-peptide complex with a size of approximately 72 kDa. In addition, the equilibrium population of the bound peptide obtained for Glu(57) was inconsistent with those for Phe(56), Glu(58), and Ile(59) and with the prothrombin/peptide ratios used in the experiments. These discrepancies can be explained by the presence of two conformations for the peptide-protein complex exchanging at a rate of approximately 100 s(-)(1). In all, our study shows that fast dissociation of protein-peptide complexes can be studied quantitatively using peptide (15)N NMR relaxation dispersion measurements without a precise knowledge of the peptide and protein concentrations. In addition, protein titration was found to improve the accuracy of quantitative analysis and may make it possible to determine the rate of conformational changes within the protein-peptide complex. 相似文献
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在产品质量判定的抽样检验问题中,当目标指标需用破坏性试验才能得其值时,更为常用的是用非破坏性试验可得量值的协变指标量来预报它。但在产品抽样验收问题上,未能形成理论较为严密的方法,这是由于预报误差这个关键问题的处理尚未解决得好,即给不出抽样方案的功效计算的正确或是近似性较好的公式。本文通过建立合理的数学模型,把对目标指标的质量要求化为对协变指标量的统计要求,从而利用两者的回归关系,结合两种复杂的抽样方案,给出功效函数的计算公式和计算方法,并进行了分析。 相似文献
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Shunli Ni Sheng Ma Yuhang Zhang Jie Yuan Haitao Yang Zouyouwei Lu Ningning Wang Jianping Sun Zhen Zhao Dong Li Shaobo Liu Hua Zhang Hui Chen Kui Jin Jinguang Cheng Li Yu Fang Zhou Xiaoli Dong Jiangping Hu Hong-Jun Gao Zhongxian Zhao 《中国物理快报》2021,(5):133-137
We systematically measure the superconducting(SC) and mixed state properties of high-quality CsV_3 Sb_5 single crystals with T_c~3.5 K.We find that the upper critical field H_(c2)(T) exhibits a large anisotropic ratio of H_(c2)~(ab)/H_(c2)~c~9 at zero temperature and fitting its temperature dependence requires a minimum two-band effective model.Moreover,the ratio of the lower critical field,H_(c1)~(ab)/H_(c1)~c,is also found to be larger than 1,which indicates that the in-plane energy dispersion is strongly renormalized near Fermi energy.Both H_(c1)(T) and SC diamagnetic signal are found to change little initially below T_c~3.5 K and then to increase abruptly upon cooling to a characteristic temperature of ~2.8 K.Furthermore,we identify a two-fold anisotropy of in-plane angular-dependent magnetoresistance in the mixed state.Interestingly,we find that,below the same characteristic T~2.8 K,the orientation of this two-fold anisotropy displays a peculiar twist by an angle of 60° characteristic of the Kagome geometry.Our results suggest an intriguing superconducting state emerging in the complex environment of Kagome lattice,which,at least,is partially driven by electron-electron correlation. 相似文献
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Broadband Sheet Parametric Oscillator for x~((2)) Optical Frequency Comb Generation via Cavity Phase Matching 下载免费PDF全文
Xin Ni Kunpeng Jia Xiaohan Wang Huaying Liu Jian Guo Shu-Wei Huang Baicheng Yao Nicolò Sernicola Zhenlin Wang Xinjie Lv Gang Zhao Zhenda Xie Shi-Ning Zhu 《中国物理快报》2021,(6):37-49
We demonstrate a broadband optical parametric oscillation, using a sheet cavity, via cavity phase-matching. A21.2 THz broad comb-like spectrum is achieved, with a uniform line spacing of 133.0 GHz, despite a relatively large dispersion of 275.4 fs~2/mm around 1064 nm. With 22.6% high slope efficiency, and 14.9 kW peak power handling, this sheet optical parametric oscillator can be further developed for x~((2)) comb. 相似文献
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We report the first amine nucleophilic approach for the modular construction of enantioenriched protected α-quaternary amino acids. The key to success is the use of an alcohol solvent, which makes a rationally designed COOMe-bonded Cu-allenylidene electrophilic intermediate stable enough to couple with amine nucleophiles before its decomposition. The reaction features wide functional group tolerance with high enantioselectivity, typically >90% ee, and is amenable to the modification of commercially available bioactive molecules. The resultant protected α-amino acids could be readily converted into a number of precious enantioenriched amines featuring α-hindered tertiary carbon centers, which are otherwise synthetically quite challenging, including those of α-amino aldehyde, peptides or α-vinyl amino ester with >92% ee in excellent yields. This protocol could be utilized for the synthesis of the protected bioactive α-ethylnorvaline in 3 steps, a significant advancement in comparison to an 11-step sequence reported previously.We report the first amine nucleophilic approach for the modular construction of enantioenriched protected α-quaternary amino acids. 相似文献
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Luhua Xiao Xiaoying Lu Huilin Yang Cuiqing Lin Le Li Chen Ni Yuan Fang Suifen Mo Ruoting Zhan Ping Yan 《Molecules (Basel, Switzerland)》2022,27(11)
In this study, the antioxidant and hypolipidemic effects of Mesona Chinensis Benth (MCB) extracts were evaluated. Seven fractions (F0, F10, F20, F30, F40, F50 and MTF) were obtained from the MCB ethanol extracts. Compared to the commercial antioxidants (vitamin C), MTF and F30 exhibited higher antioxidant activities in the antiradical activity test and the FRAP assay. The half-inhibition concentration (IC50) for MTF and F30 were 5.323 µg/mL and 5.278 µg/mL, respectively. MTF at 200 µg/mL significantly decreased the accumulation of TG in oleic acid (OA)-induced HepG2 cells and reversed the inhibitory effect of Compound C on AMPK (MTF and F30 significantly increased the glucose utilization of insulin-induced HepG2 cells). In addition, the components of MTF were identified by HPLC-MS, which were caffeic acid, quercetin 3-O-galactoside, isoquercetin, astragalin, rosmarinic acid, aromadendrin-3-O-rutinoside, rosmarinic acid-3-O-glucoside and kaempferol-7-O-glucoside. Through statistical correlations by Simca P software, it was found that the main antioxidant and hypolipidemic components of MCB might be caffeic acid, kaempferol-7-O-glucoside, rosmarinic acid-3-O-glucoside and aromadendrin-3-O-rutinoside, which may play important roles in the AMPK pathway. MTF and F30 in MCB could be potential health products for the treatment of hyperlipidemia. 相似文献