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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
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Mariam Hakami Dr. Geetanjali Deokar Jasmin Smajic Dr. Nitin M. Batra Prof. Pedro M. F. J. Costa 《化学:亚洲杂志》2021,16(11):1466-1474
In the last decade, catalytic chemical vapor deposition (CVD) has been intensively explored for the growth of single-layer graphene (SLG). Despite the scattering of guidelines and procedures, variables such as the surface texture/chemistry of catalyst metal foils, carbon feedstock, and growth process parameters have been well-scrutinized. Still, questions remain on how best to standardize the growth procedure. The possible correlation of procedures between different CVD setups is an example. Here, two thermal CVD reactors were explored to grow graphene on Cu foil. The design of these setups was entirely distinct, one being a “showerhead” cold-wall type, whereas the other represented the popular “tubular” hot-wall type. Upon standardizing the Cu foil surface, it was possible to develop a procedure for cm2-scale SLG growth that differed only by the carrier gas flow rate used in the two reactors. 相似文献
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I. F. Golovnev E. I. Golovneva L. A. Merzhievsky V. M. Fomin V. E. Panin 《Physical Mesomechanics》2015,18(3):179-186
Molecular dynamics simulation was performed to study the formation of cluster structure, interfaces, and surfaces with different curvature radii in a perfect nanocrystal passed through by a nonlinear wave. It is shown that this process is a type of nanostructure self-organization in response to an external energy flux with subsequent development of a strong rotational field. 相似文献
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Echabaane M. Hfaiedh S. Smiri B. Saidi F. Dridi C. 《Journal of Solid State Electrochemistry》2021,25(6):1797-1806
Journal of Solid State Electrochemistry - The fast and sensitive detection of copper ions would be essential for water monitoring. Herein, we report a novel development of an impedimetric sensor... 相似文献