Molina M, Segura J A, Aledo J C, Medina M A, Núnez de Castro I, Márquez J
Departament de Bioquímica y Biología Moleuclar. Facultad de Ciencias, Universidad de Málaga, Spain.
Biochem J. 1995 Jun 1;308 ( Pt 2)(Pt 2):629-33. doi: 10.1042/bj3080629.
Mitochondrial-inner-membrane vesicles, isolated from Ehrlich ascites carcinoma cells by titration with detergents, accumulated L-glutamine by a very efficient transport system. The vesicles lack any phosphate-activated glutaminase activity, allowing measurement of transport rates without interference by L-glutamine metabolism. The time course of the transport was linear for the first 60 s, reaching a steady state after 120 min. L-Glutamine transport showed co-operativity, with a Hill coefficient of 2.2; the kinetic parameters S0.5 and Vmax had values of 5 mM and 26 nmol/30 s per mg of protein respectively. The pH-dependence curve showed a bell shape, with a pH optimum about 8.0. The uptake of L-glutamine was not affected by the presence of a 50-fold molar excess of D-glutamine, L-cysteine, L-histidine, L-alanine, L-serine and L-leucine, whereas L-glutamate behaved as a poor inhibitor. The structural analogue L-glutamate gamma-hydroxamate (5mM) inhibited the net uptake by 68%; interestingly, other analogues (6-diazo-5-oxo-L-norleucine, acivicin and L-glutamate gamma-hydrazide) were ineffective. The impermeant thiol reagent p-chloromercuriphenylsulphonic acid (0.5mM) completely abolished the mitochondrial L-glutamine uptake; in contrast, other thiol reagents (mersalyl and N-ethylmaleimide) did not significantly affect the transport. These data confirm the existence of a specific transport system with high capacity for L-glutamine in the mitochondrial inner membrane, a step preceding the highly operative glutaminolysis in tumour cells.
通过用去污剂滴定从艾氏腹水癌细胞中分离出的线粒体内膜囊泡,借助一种高效的转运系统积累L-谷氨酰胺。这些囊泡缺乏任何磷酸激活的谷氨酰胺酶活性,从而能够在不受L-谷氨酰胺代谢干扰的情况下测量转运速率。转运的时间进程在前60秒呈线性,120分钟后达到稳定状态。L-谷氨酰胺转运表现出协同性,希尔系数为2.2;动力学参数S0.5和Vmax分别为5 mM和每毫克蛋白质26 nmol/30秒。pH依赖性曲线呈钟形,最适pH约为8.0。L-谷氨酰胺的摄取不受50倍摩尔过量的D-谷氨酰胺、L-半胱氨酸、L-组氨酸、L-丙氨酸、L-丝氨酸和L-亮氨酸的影响,而L-谷氨酸是一种较弱的抑制剂。结构类似物L-谷氨酸γ-羟肟酸(5 mM)使净摄取量降低68%;有趣的是,其他类似物(6-重氮-5-氧代-L-正亮氨酸、阿西维辛和L-谷氨酸γ-酰肼)无效。不透膜的硫醇试剂对氯汞苯磺酸(0.5 mM)完全消除了线粒体对L-谷氨酰胺的摄取;相比之下,其他硫醇试剂(汞撒利和N-乙基马来酰胺)对转运没有显著影响。这些数据证实了线粒体内膜中存在一种对L-谷氨酰胺具有高容量的特异性转运系统,这是肿瘤细胞中高效谷氨酰胺分解代谢之前的一个步骤。