Hajjar J J, Curran P F
J Gen Physiol. 1970 Dec;56(6):673-91. doi: 10.1085/jgp.56.6.673.
The specificity of the neutral amino acid transport system in the brush border was examined by studying the ability of amino acid analogues to inhibit the unidirectional influx of phenylalanine from mucosal solution into the cells. Effects were evaluated in terms of the affinity of various substrates for the amino acid site in the transport system. The affinity of amino acids for the site was proportional to the number of carbon atoms in the side chain. Electron-withdrawing substituents in the ring of phenylalanine increased affinity and electron-releasing groups decreased affinity. Removal of the alpha-amino group from phenylalanine decreased affinity by a factor of approximately 50 and removal of the carboxyl group decreased affinity 12-fold. Effects on affinity of variations in the side chain of the amino acid can be comparable in magnitude to that of the carboxyl group. The effect of sodium ion on the transport system appears to be similar for all compounds tested.
通过研究氨基酸类似物抑制苯丙氨酸从黏膜溶液单向流入细胞的能力,对刷状缘中中性氨基酸转运系统的特异性进行了检测。根据各种底物对转运系统中氨基酸位点的亲和力来评估其效果。氨基酸对该位点的亲和力与侧链中的碳原子数成正比。苯丙氨酸环上的吸电子取代基增加亲和力,而供电子基团则降低亲和力。从苯丙氨酸中去除α-氨基会使亲和力降低约50倍,去除羧基会使亲和力降低12倍。氨基酸侧链变化对亲和力的影响在程度上可能与羧基的影响相当。对于所有测试的化合物,钠离子对转运系统的影响似乎相似。