Bullion K, Osawa Y
Endocrine Biochemistry Department, Medical Foundation of Buffalo, Inc., NY 14203.
Endocr Res. 1988;14(1):21-33. doi: 10.1080/07435808809036337.
The initial velocity kinetics of the effect of thyroid hormone and analogs on human placental microsomal aromatase were studied. Thyroxine and its propionic analog 3,5,3',5'-tetraiodothyropropionic acid show a competitive inhibition with an apparent Ki of 1.4 microM and 8.5 microM, respectively, towards androstenedione aromatization. 3,5,3'-Triiodothyronine with a Ki of 1.8 microM shows a decreased affinity compared to thyroxine. Two analogs, 3,5,3'-triiodothyropropionic acid and 3,5,3'-triiodothyroacetic acid appear to have negligible competition.
研究了甲状腺激素及其类似物对人胎盘微粒体芳香化酶作用的初始速度动力学。甲状腺素及其丙酸类似物3,5,3',5'-四碘甲状腺丙酸对雄烯二酮芳香化分别表现出竞争性抑制，其表观抑制常数（Ki）分别为1.4微摩尔/升和8.5微摩尔/升。抑制常数为1.8微摩尔/升的3,5,3'-三碘甲状腺原氨酸与甲状腺素相比亲和力降低。两种类似物，3,5,3'-三碘甲状腺丙酸和3,5,3'-三碘甲状腺乙酸似乎竞争作用可忽略不计。
