Yamashita H, Kawakami H, Zhang Y X, Hagiwara T, Tanaka K, Nakamura S
Third Department of Internal Medicine, Hiroshima University School of Medicine, Japan.
Eur J Pharmacol. 1995 Apr 28;289(2):387-90. doi: 10.1016/0922-4106(95)90118-3.
The effects of isomers of 2-(carboxycyclopropyl)glycine (CCG) on uptake of L-glutamate were investigated in COS-7 cells that expressed a cloned human glutamate transporter (hGluT-1). The (2S, 3S, 4R)-isomer (L-CCG-III) and the (2S, 3R, 4S)-isomer (L-CCG-IV) markedly inhibited glutamate uptake with a 50% inhibitory concentration of 290 nM and 1.1 microM, respectively. The (2S, 3S, 4S)-isomer (L-CCG-I) and the (2S, 3R, 4R)-isomer (L-CCG-II) did not inhibit glutamate uptake at concentrations of < or = 10 microM. Thus, hGluT-1 showed a markedly higher affinity for L-CCG-III and L-CCG-IV with a folded conformation of the glutamate skeleton, than for L-CCG-I or L-CCG-II with an extended conformation.
在表达克隆的人类谷氨酸转运体（hGluT-1）的COS-7细胞中，研究了2-（羧基环丙基）甘氨酸（CCG）异构体对L-谷氨酸摄取的影响。（2S，3S，4R）-异构体（L-CCG-III）和（2S，3R，4S）-异构体（L-CCG-IV）显著抑制谷氨酸摄取，其50%抑制浓度分别为290 nM和1.1 μM。（2S，3S，4S）-异构体（L-CCG-I）和（2S，3R，4R）-异构体（L-CCG-II）在浓度≤10 μM时不抑制谷氨酸摄取。因此，hGluT-1对具有谷氨酸骨架折叠构象的L-CCG-III和L-CCG-IV的亲和力，明显高于对具有伸展构象的L-CCG-I或L-CCG-II的亲和力。
