Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560012, India.
Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560012, India.
Mol Cell Endocrinol. 2017 Dec 15;458:91-104. doi: 10.1016/j.mce.2017.04.006. Epub 2017 Apr 11.
Thyroid hormones (THs) play key roles in modulating the overall metabolism of the body, protein synthesis, fat metabolism, neuronal and bone growth, and cardiovascular as well as renal functions. In this review, we discuss on the thyroid hormone synthesis and activation, thyroid hormone receptors (TRs) and mechanism of action, applications of thyroid hormone analogues, particularly the compounds that are selective ligands for TRβ receptors, or enzyme inhibitors for the treatment of thyroidal disorders with a specific focus on thyroid peroxidase and iodothyronine deiodinases. We also discuss on the development of small-molecule deiodinase mimetics and their mechanism of deiodination, as these compounds have the potential to regulate the thyroid hormone levels.
甲状腺激素（THs）在调节全身代谢、蛋白质合成、脂肪代谢、神经元和骨骼生长以及心血管和肾脏功能方面发挥着关键作用。在这篇综述中，我们讨论了甲状腺激素的合成和激活、甲状腺激素受体（TRs）和作用机制、甲状腺激素类似物的应用，特别是那些对 TRβ 受体具有选择性配体的化合物，或用于治疗甲状腺疾病的酶抑制剂，特别关注甲状腺过氧化物酶和碘甲状腺原氨酸脱碘酶。我们还讨论了小分子脱碘酶模拟物的开发及其脱碘机制，因为这些化合物有可能调节甲状腺激素水平。
