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Изучение биологической активности нового нейтрального антагониста рецептора тиреотропного гормона на основе тиено[2,3-d]-пиримидина. / Деркач, К.В.; Фокина, Е.А.; Бахтюков, А.А. ; Сорокоумов, В.Н.; Степочкина, А.М.; Захарова, И.О.; Шпаков, А.О.

в: БЮЛЛЕТЕНЬ ЭКСПЕРИМЕНТАЛЬНОЙ БИОЛОГИИ И МЕДИЦИНЫ, Том 172, № 12, 12.2021, стр. 711-715.

Результаты исследований: Научные публикации в периодических изданияхстатьяРецензирование

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@article{f4391aac658d4d12b2186cf60ddabf8e,
title = "Изучение биологической активности нового нейтрального антагониста рецептора тиреотропного гормона на основе тиено[2,3-d]-пиримидина",
abstract = "A promising direction in the treatment of autoimmune hyperthyroidism is the development of low-molecular-weight antagonists of thyroid-stimulating hormone (TSH) receptor. The effect of the thieno[2,3-d]-pyrimidine derivative TPY1 on TSH-stimulated synthesis of thyroid hormones in the culture of FRTL-5 thyrocytes and on thyroliberin-stimulated production of thyroid hormones in rat blood was studied. Preincubation of FRTL-5 cells with TPY1 suppressed the stimulatory effect of TSH on the thyroxine and triiodothyronine synthesis. When administered to rats, TPY1 (i.p., 25 mg/kg) reduced thyroliberin-stimulated levels of thyroid hormones in the blood, and in the thyroid gland inhibited the gene expression of thyroid peroxidase, thyroglobulin, and Na+/I—-cotransporter responsible for thyroxine synthesis. In the absence of thyroliberin stimulation, TPY1 did not affect thyroid hormone levels and expression of thyroidogenesis genes. Thus, a new TPY1 antagonist of TSH receptor has been developed, which can become a prototype of a drug for the treatment of autoimmune hyperthyroidism.",
keywords = "аутоиммунный гипертиреоз, тиреоидный гормон, рецептор тиреотропного гормона, аллостерический антагонист, тиролиберин, autoimmune hyperthyroidism, thyroid hormone, thyroid-stimulating hormone receptor, allosteric antagonist, thyroliberin",
author = "К.В. Деркач and Е.А. Фокина and А.А. Бахтюков and В.Н. Сорокоумов and А.М. Степочкина and И.О. Захарова and А.О. Шпаков",
year = "2021",
month = dec,
language = "русский",
volume = "172",
pages = "711--715",
journal = "БЮЛЛЕТЕНЬ ЭКСПЕРИМЕНТАЛЬНОЙ БИОЛОГИИ И МЕДИЦИНЫ",
issn = "0365-9615",
publisher = "Российская академия медицинских наук",
number = "12",

}

RIS

TY - JOUR

T1 - Изучение биологической активности нового нейтрального антагониста рецептора тиреотропного гормона на основе тиено[2,3-d]-пиримидина

AU - Деркач, К.В.

AU - Фокина, Е.А.

AU - Бахтюков, А.А.

AU - Сорокоумов, В.Н.

AU - Степочкина, А.М.

AU - Захарова, И.О.

AU - Шпаков, А.О.

PY - 2021/12

Y1 - 2021/12

N2 - A promising direction in the treatment of autoimmune hyperthyroidism is the development of low-molecular-weight antagonists of thyroid-stimulating hormone (TSH) receptor. The effect of the thieno[2,3-d]-pyrimidine derivative TPY1 on TSH-stimulated synthesis of thyroid hormones in the culture of FRTL-5 thyrocytes and on thyroliberin-stimulated production of thyroid hormones in rat blood was studied. Preincubation of FRTL-5 cells with TPY1 suppressed the stimulatory effect of TSH on the thyroxine and triiodothyronine synthesis. When administered to rats, TPY1 (i.p., 25 mg/kg) reduced thyroliberin-stimulated levels of thyroid hormones in the blood, and in the thyroid gland inhibited the gene expression of thyroid peroxidase, thyroglobulin, and Na+/I—-cotransporter responsible for thyroxine synthesis. In the absence of thyroliberin stimulation, TPY1 did not affect thyroid hormone levels and expression of thyroidogenesis genes. Thus, a new TPY1 antagonist of TSH receptor has been developed, which can become a prototype of a drug for the treatment of autoimmune hyperthyroidism.

AB - A promising direction in the treatment of autoimmune hyperthyroidism is the development of low-molecular-weight antagonists of thyroid-stimulating hormone (TSH) receptor. The effect of the thieno[2,3-d]-pyrimidine derivative TPY1 on TSH-stimulated synthesis of thyroid hormones in the culture of FRTL-5 thyrocytes and on thyroliberin-stimulated production of thyroid hormones in rat blood was studied. Preincubation of FRTL-5 cells with TPY1 suppressed the stimulatory effect of TSH on the thyroxine and triiodothyronine synthesis. When administered to rats, TPY1 (i.p., 25 mg/kg) reduced thyroliberin-stimulated levels of thyroid hormones in the blood, and in the thyroid gland inhibited the gene expression of thyroid peroxidase, thyroglobulin, and Na+/I—-cotransporter responsible for thyroxine synthesis. In the absence of thyroliberin stimulation, TPY1 did not affect thyroid hormone levels and expression of thyroidogenesis genes. Thus, a new TPY1 antagonist of TSH receptor has been developed, which can become a prototype of a drug for the treatment of autoimmune hyperthyroidism.

KW - аутоиммунный гипертиреоз

KW - тиреоидный гормон

KW - рецептор тиреотропного гормона

KW - аллостерический антагонист

KW - тиролиберин

KW - autoimmune hyperthyroidism

KW - thyroid hormone

KW - thyroid-stimulating hormone receptor

KW - allosteric antagonist

KW - thyroliberin

UR - https://www.elibrary.ru/item.asp?id=47372247

M3 - статья

VL - 172

SP - 711

EP - 715

JO - БЮЛЛЕТЕНЬ ЭКСПЕРИМЕНТАЛЬНОЙ БИОЛОГИИ И МЕДИЦИНЫ

JF - БЮЛЛЕТЕНЬ ЭКСПЕРИМЕНТАЛЬНОЙ БИОЛОГИИ И МЕДИЦИНЫ

SN - 0365-9615

IS - 12

ER -

ID: 91880950