4-aminomethylbenzoic acid is a non-translocated competitive inhibitor of the epithelial peptide transporter PepT1
4-aminomethylbenzoic acid is a non-translocated competitive inhibitor of the epithelial peptide transporter PepT1
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DOI：
10.1111/j.1469-7793.1998.629bd.x
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发表时间：
1998-11-01
影响因子：
5.5
通讯作者：
Temple, CS
中科院分区：
文献类型：
--
作者：
Meredith, D;Boyd, CAR;Temple, CS
1.4-氨基甲基苯甲酸是一种模拟二肽空间构型的分子，它竞争性地抑制表达兔PepT1的非洲爪哇卵母细胞中的多肽内流，以及通过大鼠肾刷状缘膜囊泡中的PepT1内流。在表达PepT1的卵母细胞中，该分子没有通过PepT1转运，在表达PepT1的卵母细胞中，也没有间接地通过PepT1反式刺激标记的多肽在卵母细胞和肾膜囊泡中外流。然而，4-氨基甲基苯甲酸通过非标记多肽诱导的标记多肽外流的PepT1的表达来逆转反式刺激。定量上，这种逆转与竞争结合在PepT1.4外表面的4-氨基甲基苯甲酸是相容的。因此，4-氨甲基苯甲酸(第一个被发现是质子偶联寡肽转运的非移位竞争性抑制剂)及其衍生物作为实验工具可能特别有用。
1. 4-Aminomethylbenzoic acid, a molecule which mimics the spatial configuration of a dipeptide, competitively inhibits peptide influx in both Xenopus laevis oocytes expressing rabbit PepT1 and through PepT1 in rat renal brush border membrane vesicles.2. This molecule is not translocated through PepT1 as measured both by direct HPLC analysis in PepT1-expressing oocytes and indirectly by its failure to trans-stimulate labelled peptide efflux through PepT1 in oocytes and in renal membrane vesicles.3. However 4-aminomethylbenzoic acid does reverse trans-stimulation through expressed PepT1 of labelled peptide efflux induced by unlablled peptide. Quantitatively this reversal is compatible with 4-aminomethylbenzoic acid competitively binding to the external surface of PepT1.4. 4-Aminomethylbenzoic acid (the first molecule discovered to be a non-translocated competitive inhibitor of proton-coupled oligopeptide transport) and its derivatives may thus be particularly useful as experimental tools.