Supramolecular polymers based on quadruplex formation of ditopic guanosine macromonomers in non-aqueous media

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• 作者：G. Pint&#xe9 ; r ; G. Batta ; P. Horv&#xe1 ; th ; I. Lö ; ki ; T. Kurt&#xe1 ; n ; S. Antus ; S. K&#xe9 ; ki ; M. Zsuga ; G. Nagy ; J. Aradi ; T. Gunda ; P. Herczegh
• 关键词：PEPT1 ; PEPT2 ; Peptide mimics ; Drug delivery
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2007
• 期刊代码：15_09280987
• 类别：pha
• 出版时间：September 2007
• 卷：32
• 期：1, Supplement 1
• 页码：S32
• 文件大小：56 K

摘要

The H⁺/peptide cotransporters PEPT1 and PEPT2 have gained considerable interest in pharmaceutical sciences as routes for drug delivery. It is, therefore, of interest to develop uncommon artificial substrates for the two carriers. This study was initiated to investigate the binding affinity of 2-aminothiazole-4-acetic acid (ATAA) conjugates with amino acids to PEPT1 and PEPT2. The 2-aminothiazole-4-acetic acid derivatives have been synthesised and tested for their affinity to PEPT1 and PEPT2. The K_i values were compared with in silico predicted values from CoMSIA models. C-terminal ATAA-Xaa conjugates proved to be low to medium inhibitors of the [¹⁴C]Gly-Sar uptake at both carrier systems whereas N-terminal Xaa-ATAA conjugates exhibited medium to high affinity. A promising candidate for further functionalisation is Val-ATAA which shows extraordinary high affinity to PEPT1.