Gambini A, Crosti P, Bianchetti R
Biochim Biophys Acta. 1980;613(1):73-8. doi: 10.1016/0005-2744(80)90193-x.
Inhibitor studies of the only known eukaryotic methionyl-tRNA transformylase (10-formyltetrahydrofolate:L-methionyl-tRNA N-transformylase, EC 2.1.2.9) were carried out. All the natural pteroylglutamic acid derivatives examined, with the exception of pteroylglutamic acid, are inhibitors. The most effective is 5-methyltetrahydrofolate (5-CH3-H4PteGlu) (KI = 3 . 10(-6) M), which is the only noncompetitive inhibitor of the enzyme. All the other derivatives tested are competitive, and H4PteGlu shows a cooperative inhibition. These and other data obtained with pteroylglutamic analogues show that, in contrast to the bacterial enzyme, Euglena transformylase is also inhibited by compounds without a fully reduced pyrazine ring and is very sensitive to compounds with a methyl group in position 5 or 10 of the pteridine ring.
对唯一已知的真核甲硫氨酰 - tRNA转甲酰基酶（10 - 甲酰四氢叶酸：L - 甲硫氨酰 - tRNA N - 转甲酰基酶，EC 2.1.2.9）进行了抑制剂研究。除蝶酰谷氨酸外，所有检测的天然蝶酰谷氨酸衍生物均为抑制剂。最有效的是5 - 甲基四氢叶酸（5 - CH3 - H4PteGlu）（KI = 3×10⁻⁶ M），它是该酶唯一的非竞争性抑制剂。所有其他测试衍生物均为竞争性抑制剂，且H4PteGlu表现出协同抑制作用。这些以及用蝶酰谷氨酸类似物获得的其他数据表明，与细菌酶不同，眼虫转甲酰基酶也受到吡嗪环未完全还原的化合物的抑制，并且对蝶啶环5位或10位带有甲基的化合物非常敏感。
