Tisdale M J
Chem Biol Interact. 1981 Feb;34(1):75-83. doi: 10.1016/0009-2797(81)90092-2.
The tumour growth inhibitor L-2-amino-4-methoxy-trans-3-butenoic acid (Ro07-7957) inhibits serine hydroxymethyltransferase in cytosolic extracts of Walker carcinoma non-competitively with respect to L-serine with an apparent inhibition constant similar to the Km-value for L-serine. The kinetics of inactivation suggest that it reacts as an irreversible substrate analogue. Incubation of Walker cells with Ro07-7957 causes an increase in serine hydroxymethyltransferase activity which is most pronounced at concentrations less than or equal to LD50. This increase in enzyme activity does not occur in the presence of cycloheximide. These results suggest that inhibition of serine hydroxymethyltransferase in intact cells is accompanied by an increase in enzyme biosynthesis and that the growth inhibitory property or Ro07-7957 does not involve interference with the conversion of serine to glycine.
肿瘤生长抑制剂L-2-氨基-4-甲氧基反式-3-丁烯酸（Ro07-7957）在沃克癌胞质提取物中对丝氨酸羟甲基转移酶具有非竞争性抑制作用，相对于L-丝氨酸的表观抑制常数与L-丝氨酸的Km值相似。失活动力学表明它作为不可逆的底物类似物起反应。用Ro07-7957孵育沃克细胞会导致丝氨酸羟甲基转移酶活性增加，在浓度小于或等于半数致死剂量时最为明显。在存在环己酰亚胺的情况下，这种酶活性的增加不会发生。这些结果表明，完整细胞中丝氨酸羟甲基转移酶的抑制伴随着酶生物合成的增加，并且Ro07-7957的生长抑制特性不涉及对丝氨酸向甘氨酸转化的干扰。
