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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport
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B. Sc. Eduard Puig Prof. Dr. Beat Ernst Prof. Dr. Horst Kessler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8023-8027
Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (Papp) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature. 相似文献
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We give a sheaf theoretic interpretation of Potts models with external magnetic field, in terms of constructible sheaves and their Euler characteristics. We show that the polynomial countability question for the hypersurfaces defined by the vanishing of the partition function is affected by changes in the magnetic field: elementary examples suffice to see non-polynomially countable cases that become polynomially countable after a perturbation of the magnetic field. The same recursive formula for the Grothendieck classes, under edge-doubling operations, holds as in the case without magnetic field, but the closed formulae for specific examples like banana graphs differ in the presence of magnetic field. We give examples of computation of the Euler characteristic with compact support, for the set of real zeros, and find a similar exponential growth with the size of the graph. This can be viewed as a measure of topological and algorithmic complexity. We also consider the computational complexity question for evaluations of the polynomial, and show both tractable and NP-hard examples, using dynamic programming. 相似文献
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《中国物理 B》2021,30(5):56201-056201
A new three-dimensional(3 D) cellular model based on hinging open-cell Kelvin structure is proposed for its negative compressibility property. It is shown that this model has adjustable compressibility and does exhibit negative compressibility for some certain conformations. And further study shows that the images of compressibility are symmetrical about the certain lines, which indicates that the mechanical properties of the model in the three axial directions are interchangeable and the model itself has a certain geometric symmetry. A comparison of the Kelvin model with its anisotropic form with the dodecahedron model shows that the Kelvin model has stronger negative compressibility property in all three directions.Therefore, a new and potential method to improve negative compressibility property can be derived by selecting the system type with lower symmetry and increasing the number of geometric parameters. 相似文献
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文章分析了人工免疫系统的原理,简单建立了一种基于否定选择算法的网络入侵检测系统,引入了一种用于异常事件识别的r-字符块匹配规则,并对规则存在的漏洞进行了分析。 相似文献
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目标RCS动态数据的分布特征研究 总被引:1,自引:0,他引:1
复杂目标在不同视向的RCS分布特征是不同的,传统模型对此都没有给出详细的结果。文中以某歼击机和直升机为对象,应用X^2。分布、对数正态分布和瑞利分布模型,以及Kolmogomv拟合优度检验方法,研究其RCS动态测量数据的统计分布特征,得到了在一定显著性水平下,两种目标在不同视向角下对三种模型的拟合效果,同时得到应用X^2。分布拟合时模型半自由度随视向角的分布情况。在显著性水平为0.05时,对于在较短时间内录得的复杂目标动态RCS数据,应用X^2分布可以取得较好的拟合效果。文中结果精确地描述了目标RCS的起伏特征,能够为目标回波的精确模拟与检测提供可靠的依据。 相似文献
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硅光电负阻器件的构成原理与分类 总被引:1,自引:0,他引:1
郭维廉 《固体电子学研究与进展》2002,22(1):120-126
将三端负阻器件与硅光电探测器相结合 ,通过新的构思成功地提出并构成了一类新型光电器件——硅光电负阻器件。文中报道了该器件构成的一般性原理 ,以及依据此构成原理确定的分类方法 相似文献
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We introduce the notion of an invariant of characteristics for a system of first-order partial differential equations. We prove that the existence of invariants is connected with passiveness of some systems. We describe a few methods for construction of new invariants from those already known. We give a scheme for application of the invariants to reduction and integration of systems of partial differential equations. As an application we consider the equation of gas dynamics. 相似文献