Preparation of tritium labeled dexamethasone phosphate and its application to assess the affinity of ligands to glucocorticoid receptors

封面

如何引用文章

全文:

开放存取 开放存取
受限制的访问 ##reader.subscriptionAccessGranted##
受限制的访问 订阅存取

详细

The possibility of introducing tritium using the thermal activation method into dexamethasone and dexamethasone phosphate has been shown. Labeled compounds have been successfully used to assess the affinity of ligands to glucocorticoid receptors.

全文:

受限制的访问

作者简介

G. Badun

Moscow State University

编辑信件的主要联系方式.
Email: badunga@my.msu.ru

Faculty of Chemistry

俄罗斯联邦, Moscow, 119991

E. Zhidkova

Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Email: badunga@my.msu.ru
俄罗斯联邦, Moscow, 115478

M. Chernysheva

Moscow State University

Email: badunga@my.msu.ru

Faculty of Chemistry

俄罗斯联邦, Moscow, 119991

A. Enikeev

Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Email: badunga@my.msu.ru
俄罗斯联邦, Moscow, 115478

M. Yakubovskaya

Blokhin Russian Cancer Research Center, Ministry of Health of Russia; Friendship University of Russia

Email: badunga@my.msu.ru
俄罗斯联邦, Moscow, 115478; Moscow, 117198

E. Lesovaya

Blokhin Russian Cancer Research Center, Ministry of Health of Russia; Friendship University of Russia; Pavlov Ryazan State Medical University, Ministry of Health of Russia

Email: badunga@my.msu.ru
俄罗斯联邦, Moscow, 115478; Moscow, 117198; Ryazan, 390026

参考

  1. Atzrodt J., Derdau V., Kerr W.J., Reid M. // Angew. Chem. Int. Ed. 2018. Vol. 57. P. 1758–1784.
  2. Kopf S., Bourriquen F., Li W., Neumann H., Junge K., Beller M. // Chem. Rev. 2022. Vol. 122. P. 6634−6718.
  3. Шевченко В.П., Нагаев И.Ю., Мясоедов Н.Ф. // Радиохимия. 2022. Т. 64. № 4. С. 303–349.
  4. Бадун Г.А., Чернышева М.Г. // Радиохимия. 2023. Т. 65. № 2. С. 158–171.
  5. Kadmiel M., Cidlowski J.A. // Trends Pharmacol. Sci. 2013. Vol. 34. N 9. P. 518–530.
  6. Ramamoorthy S., Cidlowski J.A. // Rheum. Dis. Clin. N. Am. 2016. Vol. 42. N 1. P. 15–31.
  7. Lesovaya E., Yemelyanov A., Swart A.C., Swart P., Haegeman G., Budunova I. // Oncotarget. 2015. Vol. 6. N 31. P. 30730–30744.
  8. De Bosscher K., Haegeman G., Elewaut D. // Curr. Opin. Pharmacol. 2010. Vol. 10. N 4. P. 497–504.
  9. De Bosscher K., Beck I.M., Ratman D., Berghe W.V., Libert C. // Trends Pharmacol. Sci. 2016. Vol. 37. N 1. P. 4–16.
  10. Lesovaya E.A., Chudakova D., Baida G., Zhidkova E.M., Kirsanov K.I., Yakubovskaya M.G., Budunova I.V. // Oncotarget. 2022. Vol. 13. P. 408–424.
  11. De Bosscher K. // J. Steroid Biochem. Mol. Biol. 2010. Vol. 120. N 2–3. P. 96–104.
  12. Lesovaya E.A., Kirsanov K.I., Popa A., Belitsky G.A., Yakubovskaya M.G., Gordon L.I., Rosen S.T., Budunova I.V. // Cell Cycle. 2013. Vol. 12. N 1. P. 133–144.
  13. Edvinsson Å., Hoyer A., Hansson M., Kallak T.K., Sundström-Poromaa I., Skalkidou A., Lager S. // Ups. J. Med. Sci. 2020. Vol. 125. N 1. P. 30–36.
  14. Lesovaya E.A., Yemelyanov A.Yu., Kirsanov K.I., Yakubovskaya M.G., Budunova I.V. // Biochem. Mosc. 2011. Vol. 76. N 11. P. 1242–1252.
  15. Souffriau J., Eggermont M., Van Ryckeghe, S., Van Looveren K., Van Wyngene L., Van Hamme E., Vuylsteke M., Beyaert R., De Bosscher K., Libert C. // Sci. Rep. 2018. Vol. 8. N. 1. ID 12894.
  16. Nishi M., Ogawa H., Ito T., Matsuda K.-I., Kawata M. // Mol. Endocrinol. 2001. Vol. 15. N 7. P. 1077–1092.
  17. Chen T., Xie W., Agler M., Banks M. // Assay Drug Dev. Technol. 2003. Vol. 1. N 6. P. 835–842.
  18. Seo J.H., Jin M.H., Chang Y.H. // BMC Complement. Med. Ther. 2020. Vol. 20. N 1. ID 176.
  19. Miner J.N., Tyree C., Hu J., Berger E., Marschke K., Nakane M., Coghlan M.J., Clemm D., Lane B., Rosen J. // Mol. Endocrinol. Vol. 17. N 1. P. 117–127.
  20. West D. C., Kocherginsky M., Tonsing-Carter E. Y., Dolcen D. N., Hosfield D. J., Lastra R. R., Sinnwell J.P, Thompson K.J., Bowie K.R., Harkless R.V., Skor M.N., Pierce C.F., Styke S.C., Kim C.R., de Wet L., Greene G.L., Boughey J.C., Goetz M.P., Kalari K.R., Wang L., Fleming G.F., Györffy B., Conzen, S. D. // Clin. Cancer Res. 2018. Vol. 24. N 14. P. 3433–3446.
  21. He X., Zhao W., Yao L., Sun P., Cheng G., Liu Y., Yu Y., Liu Y., Wang T., Zhang Q., Qin L., Zhang Q. // Phytomedicine. 2023. Vol. 119. ID 154953.
  22. Bain D.L., Yang Q., Connaghan K.D., Robblee J.P., Miura M.T., Degala G.D., Lambert J.R., Maluf N.K. // J. Mol. Biol. Vol. 2012. Vol. 422. N 1. P. 18–32.
  23. Bledsoe R.K., Montana V.G., Stanley T.B., Delves C.J., Apolito C.J., McKee D.D., Consler T.G., Parks D.J., Stewart E.L., Willson T.M., Lambert M.H., Moore J.T., Pearce K.H., Xu H.E. // Cell. 2002. Vol. 110. N 1. P. 93–105.
  24. Maguire J.J., Kuc R.E., Davenport A.P. // Meth. Mol. Biol. 2012. Vol. 897. P. 31–77.
  25. Шэнь Т., Чернышева М.Г., Бадун Г.А. // Радиохимия. 2023. Т. 65. № 6. С. 575-583.
  26. Бадун Г.А., Мясников И.Ю., Казаков А.Г., Федорова Н.В., Чернышева М.Г. // Радиохимия. 2019. Т. 61. № 2. С. 168–173.
  27. De Bosscher K., Berghe W.V., Beck I.M., Van Molle W., Hennuyer N., Hapgood J., Libert C., Staels B., Louw A., Haegeman G. // Proc. Natl. Acad. Sci. 2005. Vol. 102. N 44. P. 15827–15832.
  28. Yemelyanov A., Czwornog J., Gera L., Joshi S., Chatterton R.T., Budunova I. // Cancer Res. 2008. Vol. 68. N 12. P. 4763–4773.

补充文件

附件文件
动作
1. JATS XML
下载
2. Scheme 1. Glucocorticoid receptor ligands used in the work: a – dexamethasone, b – dexamethasone phosphate, c – Compound A (CpdA).

下载 (83KB)
索引源数据
3. Fig. 1. Dependence of the specific radioactivity of [3H]dexamethasone on the mass of the drug applied to the walls of the reaction vessel from a methanol solution.

下载 (76KB)
索引源数据
4. Fig. 2. Dependence of the specific radioactivity of [3H]dexamethasone phosphate on the temperature of the atomizer when the substance is applied to smooth walls by lyophilization of an aqueous solution (1) and by evaporation of a methanol solution applied to rough walls of the reaction vessel (2).

下载 (85KB)
索引源数据
5. Fig. 3. Dependence of the signal level (in % of the maximum) on the incubation time with [3H]dexamethasone.

下载 (79KB)
索引源数据
6. Fig. 4. Change in the proportion of [3H]dexamethasone bound to GH at its concentration of 0.5, 1 and 2 μmol/l and different amounts of unlabeled dexamethasone phosphate. Incubation time 90 min.

下载 (60KB)
索引源数据
7. Fig. 5. Dependence of the proportion of GH-bound [3H]dexamethasone phosphate (0.5 μmol/L) on GH in the presence of unlabeled dexamethasone phosphate or CpdA. Incubation time is 90 min. Data are presented as % of the signal level in samples with [3H]dexamethasone.

下载 (53KB)
索引源数据

版权所有 © Russian Academy of Sciences, 2024