Remarkable Effect of Chalcogen Substitution on an Enzyme Mimetic for Deiodination of Thyroid Hormones
作者:Karuppusamy Raja、Govindasamy Mugesh
DOI:10.1002/anie.201502762
日期:2015.6.22
Iodothyronine deiodinases are selenoenzymes which regulate the thyroid hormone homeostasis by catalyzing the regioselective deiodination of thyroxine (T4). Synthetic deiodinase mimetics are important not only to understand the mechanism of enzyme catalysis, but also to develop therapeutic agents as abnormal thyroid hormone levels have implications in different diseases, such as hypoxia, myocardial
碘甲状腺素脱碘酶是通过催化甲状腺素(T4)的区域选择性脱碘作用来调节甲状腺激素稳态的硒酶。合成的脱碘酶模拟物不仅对于了解酶催化的机理很重要,而且对于开发治疗剂也很重要,因为甲状腺激素水平异常会影响不同疾病的发生,例如缺氧,心肌梗塞,危重疾病,神经元缺血,组织损伤和癌症。本文描述的是,通过碲置换一系列脱碘酶模拟物中的硫/硒原子显着改变了对T4的反应性和区域选择性。