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2.
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
3.
Eduard Feireisl Antonín Novotný Hana Petzeltov 《Mathematical Methods in the Applied Sciences》2002,25(12):1045-1073
We prove a general compactness result for the solution set of the compressible Navier–Stokes equations with respect to the variation of the underlying spatial domain. Among various corollaries, we then prove a general existence theorem for the system in question with no restrictions on smoothness of the spatial domain. Copyright © 2002 John Wiley & Sons, Ltd. 相似文献
4.
This paper solves the problem of the duration of the total eclipseof a satellite of a body, provided that (a) the body is sphericalin shape and the mass distribution inside the body is sphericallysymmetrical; (b) the satellite is a very small object; (c) thesatellite's orbit around a body is circular and the satellitecan pass through the centre of its shadow; (d) a source of lightis the source of the conical body's shadow (umbra) and it doesnot change its apparent position in the sky; (e) there are noperturbations on the satellite's orbit. The solution presentedrepresents the general discussion of the problem based on utilizationof some parts of the theory of contraction mappings. 相似文献
5.
Eduard Prugovečki 《Foundations of Physics》1991,21(1):93-124
The issue of the intrinsic nonlocality of quantum mechanics raised by J. S. Bell is examined from the point of view of the recently developed method of geometro-stochastic quantization and its applications to general relativistic quantum theory. This analysis reveals that a distinction should be made between the topological concept of locality used in formulating relativistic causality and a type of geometric locality based on the concept of fiber bundle, which can be used in extending the strong equivalence principle to the quantum domain. Both play an essential role in formulating a notion of geometro-stochastic propagation based on quantum diffusions, which throws new light on the EPR paradox, on the origin of the arrow of time, and on other fundamental issues in quantum cosmology and the theory of measurement. 相似文献
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Quantitative H–Al distances in acid sites of two zeolites with MFI and IFR framework topology were obtained by numerical simulation of 1H{27Al} rotational echo adiabatic passage double resonance (REAPDOR) experiments. A 27Al offset-dependent data set yields for each resolved 1H NMR line a corresponding nuclear electric quadrupole coupling constant of the neighboring 27Al site. This information is used for analyzing a second data set for on-resonance irradiation, where the dipolar evolution time (number of rotor cycles) was varied, to yield the 1H–27Al dipolar coupling constant. Numerical simulations indicate that the REAPDOR method does not depend significantly on the polar angles, defining the orientation of the electric field gradient tensor of 27Al with respect to the Al–H dipolar vector. In contrast, the transfer of populations in double resonance sequence is sensitive to these angles, and it can be thus used to measure them. 相似文献
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In this paper we construct a positive doubly power bounded operator
with a nonpositive inverse on an AL-space. 相似文献
10.
R. Resel M. Oehzelt O. Lengyel T.U. Schülli G. Hlawacek C. Teichert G. Koller 《Surface science》2006,600(19):4645-4649
A para-sexiphenyl monolayer of near up-right standing molecules (nominal thickness of 30 Å) is investigated in-situ by X-ray diffraction using synchrotron radiation and ex-situ by atomic force microscopy. A terrace like morphology is observed, the step height between the terraces is approximately one molecular length. The monolayer terraces, larger than 20 μm in size, are extended along the [0 0 1] direction of the TiO2(1 1 0) substrate i.e. along the Ti-O rows of the reconstructed substrate surface. The structure of the monolayer and its epitaxial relationship to the substrate is determined by grazing incidence X-ray diffraction. Extremely sharp diffraction peaks reveal high crystalline order within the monolayer, which was found to have the bulk structure of sexiphenyl. The monolayer terraces are epitaxially oriented with the (0 0 1) plane parallel to the substrate surface (out-of-plane order). Four epitaxial relationships are observed. This in-plane alignment is determined by the arrangement of the terminal phenyl rings of the sexiphenyl molecules parallel to the oxygen rows of the substrate. 相似文献