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РЖ ВИНИТИ 34 (BI48) 96.12-04Т2.212

The selenium analog of 6-propylthiouracil. Measurement of its inhibitory effect on type I iodothyronine deiodinase and of its antithyroid activity [Text] / Alvin Taurog [et al.] // Biochem. Pharmacol. - 1995. - Vol. 49, N 5. - P701-709 . - ISSN 0006-2952
Перевод заглавия: Селеновое производное 6-пропилтиоурацила. Определение ингибирующей активности на йодтирониндейодиназу типа I и антитиреоидная активность
Аннотация: Propylthiouracil (PTU), a widely used antithyroid drug for the treatment of Graves' disease, is also a potent inhibitor of Type I iodothyronine deiodinase (ID-1). Inhibition of ID-1 was attributed initially to the formation of a mixed disulfide between PTU and a putative cysteine residue at the active site. It has been demonstrated recently that ID-1 is a selenium-containing enzyme, with selenocysteine, rather than cysteine, at the active site. It seemed possible, therefore, that the selenium analog of PTU (PSeU) might be a more potent inhibitor of ID-1 than PTU. To test this possibility, we developed a procedure for the synthesis of PSeU, and we compared PSeU and PTU as inhibitors of ID-1 in a test system containing {125}I-rT[3], rat liver microsomes, and dithiothreitol. Deiodinase activity was measured by the increase in {125}I-iodide. PTU and PSeU were tested at 0.1, 0.3, 1 and 3 'мю'M. Based on results of four separate experiments, the drugs were essentially equipotent as inhibitors of ID-1, although statistical analysis suggested that PSeU may be slightly more potent than PTU. PTU and PSeU were also compared for antithyroid activity in vivo. As inhibitors of the catalytic activity of thyroid peroxidase (TPO), the two drugs were essentially equipotent in iodination and guaiacol assays involving measurements made shortly after the addition of H[2]O[2]. However, in in vivo experiments with rats, PSeU showed no appreciable inhibition of organic iodine formation in the thyroid, whereas PTU, as expected, was a potent inhibitor. The lack of inhibition of organic iodine formation in vivo by PSeU suggests that, unlike PTU, it is not concentrated by the thyroid gland. In an iodination system in which H[2]O[2] was generated by glucose-glucose oxidase, both PTU and PSeU, when present at 10 'мю'M, acted as reversible inhibitors of iodination. However, when the drug concentration was raised to 50 'мю'M, TPO was inactivated and iodination was irreversibly inhibited. These results suggest that PTU and PSeU inhibit TPO-catalyzed iodination by similar mechanisms. Библ. 17

ГРНТИ	34.45.21

ВИНИТИ 341.45.21.65.21
Рубрики: АНТИТИРЕОИДНЫЕ СРЕДСТВА
ПРОПИЛТИОУРАЦИЛ* 6-
СЕЛЕНОВОЕ ПРОИЗВОДНОЕ
ЙОДТИРОНИНДЕЙОДИНАЗА ТИПА I

Доп.точки доступа:
Taurog, Alvin; Dorris, martha L.; Hu, Wei-Xiao; Guziec, Frank S.

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