Snell K, Riches D
Department of Biochemistry, University of Surrey, Guildford, U.K.
Cancer Lett. 1989 Mar;44(3):217-20. doi: 10.1016/0304-3835(89)90064-5.
The effect of the triazine antifolate NSC 127755 on serine hydroxymethyltransferase activity in mouse myeloma X63 cells in culture was determined. The enzyme was inhibited, apparently irreversibly, with IC50 approximately 5 X 10(-8) M. A similar concentration-dependency for inhibition of [6-3H]deoxyuridine incorporation into DNA was observed in these cells in culture. Long-term culture of myeloma cells with NSC 127755 resulted in a progressive decrease in the number of viable cells. The study emphasises the significance of serine hydroxymethyltransferase as a target for anticancer chemotherapy.
测定了三嗪抗叶酸剂NSC 127755对培养的小鼠骨髓瘤X63细胞中丝氨酸羟甲基转移酶活性的影响。该酶受到抑制，显然是不可逆的，IC50约为5×10^(-8)M。在这些培养的细胞中，观察到对[6-3H]脱氧尿苷掺入DNA的抑制也有类似的浓度依赖性。用NSC 127755对骨髓瘤细胞进行长期培养导致活细胞数量逐渐减少。该研究强调了丝氨酸羟甲基转移酶作为抗癌化疗靶点的重要性。
