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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport 下载免费PDF全文
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
2.
We report on the first observation and studies of a weak delocalizing logarithmic temperature dependence of the conductivity,
which causes the conductivity of the 2D metal to increase as T decreases down to 16 mK. The prefactor of the logarithmic dependence is found to decrease gradually with density, to vanish
at a critical density n
c
, 2∼2×1012 cm−2, and then to have the opposite sign at n>n
c
,2. The second critical density sets the upper limit on the existence region of the 2D metal, whereas the conductivity at the
critical point, G
c
,2∼120e
2/h, sets an upper (low-temperature) limit on its conductivity.
Pis’ma Zh. éksp. Teor. Fiz. 68, No. 6, 497–501 (25 September 1998)
Published in English in the original Russian journal. Edited by Steve Torstveit. 相似文献
3.
The association of complex formation with static quenching in CT systems was investigated. Evaluation of the data made evident
that the inner filter effect must be allowed for. Time-resolved and temperature-dependent stationary measurements of fluorescence
led to the separation of dynamic and static quenching components. The static quenching constant is discussed with respect
to the equilibrium constant of complex formation determined by absorption spectroscopy. 相似文献
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Horst Szambien 《Results in Mathematics》1992,22(1-2):619-621
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The difference in reactivity of the two modifications of InCl in solid state reactions with SnCl2 is discussed. It is explained on the basis of semi‐empirical and ab initio calculations giving the density of states diagrams of InCl and the energies of possible disproportionation reactions. Their general features are discussed on the basis of a simple bonding picture for open‐packed structures involving inert pair elements. A detailed analysis of the DOS distribution allows to pinpoint the observed redox instability to a specific structural feature of α‐InCl. 相似文献
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