Substrate specificity of human glycinamide ribonucleotide transformylase.
Substrate specificity of human glycinamide ribonucleotide transformylase.
复制标题
人甘氨酰胺核糖核苷酸转化酶的底物特异性。
DOI：
10.1006/abbi.1999.1428
复制
发表时间：
1999
影响因子：
3.9
通讯作者：
Carperelli,CA
中科院分区：
文献类型：
--
作者：
Antle,VD;Donat,N;Hua,M;Liao,PL;Vince,R;Carperelli,CA
对化疗靶点甘氨酰胺核糖核苷酸转化酶的核苷酸底物特异性进行了研究。该酶接受甘氨酰胺核糖核苷酸的肌氨酸类似物、碳环甘氨酰胺核糖核苷酸和碳环甘氨酰胺核糖核苷酸的两种膦酸酯衍生物，相对于β-甘氨酰胺核糖核苷酸获得的V/K值，V/K值分别为1、27、1.4和2.9%。其他几种类似物，即截短膦酸酯和2′，3 ′-双脱氧和2 ′，3 ′-双脱氢碳环甘氨酰胺核苷酸，都是酶的抑制剂，与甘氨酰胺核苷酸竞争，Ki值比β-甘氨酰胺核苷酸的Km值高约100倍。尽管本研究的结果与先前用禽酶（V.D. Antle，D.刘，B。R.麦凯勒角A. Caperelli，M. Hua，和R. Vince（1996）J.Biol.Chem.271，6045-6049），已经发现了两种酶种类之间的定量差异。
Thenucleotide substrate specificity of human glycinamide ribonucleotide transformylase, a chemotherapeutic target, has been examined. The enzyme accepts the sarcosyl analog of glycinamide ribonucleotide, carbocyclic glycinamide ribonucleotide, and two phosphonate derivatives of carbocyclic glycinamide ribonucleotide with V/K values, relative to that obtained for β-glycinamide ribonucleotide, of 1, 27, 1.4, and 2.9%, respectively. Several other analogs of carbocyclic glycinamide ribonucleotide, namely a truncated phosphonate and 2′,3′-dideoxy- and 2′,3′-dideoxy-2′,3′-didehydro-carbocyclic glycinamide ribonucleotide, were inhibitors of the enzyme, competitive against glycinamide ribonucleotide, with Kivalues approximately 100 times higher than the Kmfor β-glycinamide ribonucleotide. Although the results of the present study parallel those obtained previously with the avian enzyme (V. D. Antle, D. Liu, B. R. McKellar, C. A. Caperelli, M. Hua, and R. Vince (1996) J. Biol. Chem. 271, 6045–6049), quantitative differences between the two enzyme species have been uncovered.