Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560 012, India.
Bioinorg Chem Appl. 2006;2006:23214. doi: 10.1155/BCA/2006/23214. Epub 2006 Nov 12.
Propylthiouracil (PTU) and methimazole (MMI) are the most commonly used antithyroid drugs. The available data suggest that these drugs may block the thyroid hormone synthesis by inhibiting the thyroid peroxidase (TPO) or diverting oxidized iodides away from thyroglobulin. It is also known that PTU inhibits the selenocysteine-containing enzyme ID-1 by reacting with the selenenyl iodide intermediate (E-SeI). In view of the current interest in antithyroid drugs, we have recently carried out biomimetic studies to understand the mechanism by which the antithyroid drugs inhibit the thyroid hormone synthesis and found that the replacement of sulfur with selenium in MMI leads to an interesting compound that may reversibly block the thyroid hormone synthesis. Our recent results on the inhibition of lactoperoxidase (LPO)-catalyzed oxidation and iodination reactions by antithyroid drugs are described.
丙硫氧嘧啶(PTU)和甲巯咪唑(MMI)是最常用的抗甲状腺药物。现有数据表明,这些药物可能通过抑制甲状腺过氧化物酶(TPO)或使氧化碘从甲状腺球蛋白中转移来阻断甲状腺激素的合成。已知 PTU 通过与硒代亚碘酸盐中间体(E-SeI)反应来抑制含硒半胱氨酸的酶 ID-1。鉴于目前对抗甲状腺药物的兴趣,我们最近进行了仿生学研究,以了解抗甲状腺药物抑制甲状腺激素合成的机制,并发现将 MMI 中的硫替换为硒会产生一种有趣的化合物,该化合物可能可逆地阻断甲状腺激素的合成。我们最近关于抗甲状腺药物抑制乳过氧化物酶(LPO)催化的氧化和碘化反应的结果也进行了描述。