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1.
Somatostatin analogues are useful pharmaceuticals in peptide receptor radionuclide therapy. In previous studies, we analyzed a new bicyclic somatostatin analogue (BCS) in connection with Cu(II) ions. Two characteristic sites were present in the peptide chain: the receptor- and the metal-binding site. We have already shown that this ligand can form very stable imidazole complexes with the metal ion. In this work, our aim was to characterize the intramolecular interaction that occurs in the peptide molecule. Therefore, we analyzed the coordination abilities of two cyclic ligands, i.e., P1 only with the metal binding site and P2 with both sites, but without the disulfide bond. Furthermore, we used magnetic circular dichroism (MCD) spectroscopy to better understand the coordination process. We applied this method to analyze spectra of P1, P2, and BCS, which we have described previously. Additionally, we analyzed the MCD spectra of P3 ligand, which has only the receptor binding site in its structure. We have unequivocally shown that the presence of the Phe-Trp-Lys-Thr motif and the disulfide bond significantly increases the metal binding efficiency.  相似文献   
2.
Immature oils were proved to be existed in Es4u reservoirs based on GC-MS and carbon isotope analysis of oil sand and source rocks in Qingdong sag. By comprehensive discussion with compositional data from different sags in China, bicyclic sesquiterpenoids are related to thermal maturity and can be used in oil maturity identification. A new indicator, 4,4,8,9,9-pentamethyl decahydronaphthalene /8β(H)-homodrimane, is proposed for distinguishing immature and mature oils in the study area. It signifies mature when this ratio value is higher than 0.34, and immature when the value is lower than 0.34. The varying structures of the two compounds determines their stability.  相似文献   
3.
陈君  孔凡家  吴金钗 《广州化工》2011,39(15):43-45,75
对比阿培南的合成路线进行文献综述,先总体介绍比阿培南的两条总合成路线,进而介绍其中侧链对接法所涉及各关键中间体(包括1β-甲基碳青霉烯母核、吡唑烷环、含硫双五环侧链)的合成路线。1β-甲基碳青霉烯母核可通过分子内卡宾插入反应或分子内Dieckmann缩合反应两种方法合成,含硫双五环侧链则有以1,2-二(叔丁氧羰基)肼为原料和以水合肼为原料两条路线。  相似文献   
4.
Methods to access natural‐product‐like macrocyclic peptides can disclose new opportunities for the exploration of this important structural class for chemical biology and drug discovery applications. Here, the scope and mechanism of a novel strategy for directing the biosynthesis of thioether‐bridged bicyclic peptides in bacterial cells was investigated. This method entails split intein‐catalyzed head‐to‐tail cyclization of a ribosomally produced precursor peptide, combined with inter‐side‐chain crosslinking through a genetically encoded cysteine‐reactive amino acid. This strategy could be successfully applied to achieve formation of structurally diverse bicyclic peptides with high efficiency and selectivity in Escherichia coli. Insights into the sequence of reactions underlying the peptide bicyclization process were gained from time‐course experiments. Finally, the potential utility of this methodology toward the discovery of macrocyclic peptides with enhanced functional properties was demonstrated through the isolation of a bicyclic peptide with sub‐micromolar affinity for streptavidin.  相似文献   
5.
Assessment of human error in maintenance requires identification of the contributing factors that lead to human error(s). These factors are called human error inducing factors (HEIFs), which take into consideration both the active and latent error contributing aspects related to man, machine and environment. A systems approach of the Graph Theory is applied in this paper for quantifying human error in maintenance activities that models the identified factors and their interactions/interrelationships in terms of human error digraph. The nodes in the digraph represent the HEIFs and the edges represent their interrelationships. The digraph is converted into an equivalent matrix and an expression based on this is developed, which is characteristic of the human error in maintenance. This expression is used to evaluate a human error index by substituting the numerical value of the factors and their interrelations. The index is a measure of the human error potential involved in the maintenance of systems. A higher value of index indicates that the error likelihood is more for the associated tasks, and more efforts are required to make the system less prone to human error. The proposed methodology is illustrated using a case study. The approach is anticipated to play a significant role in identifying sources of human errors and predicting their impact; and will help to integrate human factors during design stage with the objective of reducing human error in maintenance. Copyright © 2011 John Wiley & Sons, Ltd.  相似文献   
6.
定义了有向图指定源点连通支配集问题。借助参数算法中的技术设计了针对该问题的规约规则,通过规约规则的实施来降低原问题的规模;随后又设计了近似算法在规约后的有向图中求出一个较小的连通支配集;最后结合规约规则带来的一些良好特性设计了优化规则,通过优化变换的实施进一步缩减由近似算法求得的连通支配集。不同模型随机图上的模拟实验表明这些规则和算法是有效的。  相似文献   
7.
利用多功能表面性能实验机考察了不同载荷下钠钙硅玻璃与45#钢对摩时的摩擦磨损性能,用体式显微镜和显微硬度计观察和分析磨损表面形貌,并利用双环实验测试了不同加载时间的钠钙硅玻璃残余强度,探讨了材料的磨损机理,结果表明:磨损率随着载荷的增加出现波动,当载荷低于10 N时,摩擦系数随载荷增加而明显增大,而当载荷超过10 N时,摩擦系数随载荷增加而明显降低,在较低载荷下,钠钙硅玻璃的磨损失效主要源于轻微点蚀,在较高载荷下,其磨损失效主要源于表层塑性变形。  相似文献   
8.
基于全油气相色谱/质谱联用定量分析技术,分析了冀中凹陷文安油田原油中双环倍半萜在空间分布上的非均质性特征及其变化规律,并讨论了其非均质性特征的地质-地球化学意义。结果表明:微生物的降解作用对双环倍半萜的影响并不明显,文安油田原油含有丰富的双环倍半萜;文安油田原油中双环倍半萜的总体分布特征是C14倍半萜化合物相对丰度最小,C15倍半萜化合物相对丰度居中,C16倍半萜化合物相对丰度最高;文安油田南区与北区原油存在明显非均质性;重排补身烷与8β(H)-补身烷、C30重排藿烷与C30藿烷、C27重排甾烷与C27甾烷的相对丰度比值具有显著相关性,反映重排补身烷的形成机理与重排甾烷、重排藿烷的形成具有相似性;原油分子组成上的非均质性预示着文安油田原油可能存在两种不同的成因类型,文安油田南区和北区可能存在着2个油气富集体系。  相似文献   
9.
研究一类特殊的本原双色有向图,其未着色的有向图包含两个圈.首先求出该双色有向图为本原时的圈矩阵,然后利用该圈矩阵和图论的有关知识,得出了这个本原双色有向图的指数集.  相似文献   
10.
This article addresses algebraic criteria for consensus problems of continuous-time networked systems with fixed and switching topology. A special eigenvector ω of the Laplacian matrix is first constructed and correlated with the connectivity of digraph. And then, some necessary and/or sufficient algebraic conditions are presented by employing the vector ω, which can directly determine whether the consensus problem can be solved. More importantly, for the switching topology case, the obtained algebraic conditions for the average consensus problem are necessary and sufficient. Furthermore, the presented results clearly show that only the agents corresponding to the positive elements of ω contribute to the group decision value and decide the collective behaviour of the system. Particularly for the fixed topology case, the role of each agent is exactly measured by the value of the corresponding element of ω. Based on these results, some extended protocols are further proposed to solve the average consensus problem, in which the interaction digraphs are not needed to be balanced. Numerical examples are included to illustrate the obtained results.  相似文献   
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