Berry M J, Kieffer J D, Harney J W, Larsen P R
Howard Hughes Medical Institute Laboratory, Department of Medicine, Brigham and Women's Hospital, Boston, Massachusetts.
J Biol Chem. 1991 Aug 5;266(22):14155-8.
The conversion of thyroxine to 3,5,3'-triiodothyronine (T3) is the first step in thyroid hormone action, and the Type I iodothyronine deiodinase supplies most of this extrathyroidal T3 in the rat. We found that the cDNA coding for this enzyme contains an in-frame UGA encoding the rare amino acid selenocysteine. Using site-directed mutagenesis, we have converted selenocysteine to cysteine and expressed the wild-type and cysteine mutant enzymes in JEG-3 cells by transient transfection. The kinetic properties of the transiently expressed wild-type enzyme are nearly identical to those reported for rat liver Type I deiodinase. Substitution of sulfur for selenium causes a 10-fold increase in the Km of the enzyme for the favored substrate 3,3',5'-triiodothyronine (rT3), a 100-fold decrease in the sensitivity of rT3 deiodination to competitive inhibition by gold and a 300-fold increase in the apparent Ki for uncompetitive inhibition by 6-n-propylthiouracil. These results demonstrate that selenium is responsible for the biochemical properties which characterize Type I iodothyronine monodeiodination.
甲状腺素转化为3,5,3'-三碘甲状腺原氨酸(T3)是甲状腺激素发挥作用的第一步,在大鼠体内,Ⅰ型碘甲状腺原氨酸脱碘酶提供了大部分的外周T3。我们发现,编码该酶的cDNA含有一个框内UGA,其编码稀有氨基酸硒代半胱氨酸。通过定点诱变,我们已将硒代半胱氨酸转化为半胱氨酸,并通过瞬时转染在JEG-3细胞中表达野生型和半胱氨酸突变型酶。瞬时表达的野生型酶的动力学特性与报道的大鼠肝脏Ⅰ型脱碘酶的动力学特性几乎相同。用硫取代硒会使该酶对偏好底物3,3',5'-三碘甲状腺原氨酸(反T3,rT3)的Km增加10倍,rT3脱碘对金竞争性抑制的敏感性降低100倍,对6-正丙基硫氧嘧啶非竞争性抑制的表观Ki增加300倍。这些结果表明,硒决定了Ⅰ型碘甲状腺原氨酸单脱碘的生化特性。