Sulfonyl-bridged Calix[4]arene as an Inhibitor of Protein Tyrosine Phosphatases
Тип публікації :
Стаття
Дата випуску :
2017
Автор(и) :
Buldenko, Vladyslav
Kobzar, Oleksandr
Trush, Viacheslav
Drapailo, Andriy
Kalchenko, Vitaly
Vovk, Andriy
Мова основного тексту :
Англійська
eKNUTSHIR URL :
Том :
5
Випуск :
2
ISSN :
2312-3222
Початкова сторінка :
144
Кінцева сторінка :
151
Цитування :
[APA 7] Buldenko, V., Kobzar, O., Trush, V., Drapailo, A., Kalchenko, V., & Vovk, A. (2017). Sulfonyl-bridged Calix[4]arene as an Inhibitor of Protein Tyrosine Phosphatases. French-Ukrainian Journal of Chemistry, 5(2), 144–151. https://doi.org/10.17721/fujcV5I2P144-151
[ДСТУ] Sulfonyl-bridged Calix[4]arene as an Inhibitor of Protein Tyrosine Phosphatases / V. Buldenko et al. French-Ukrainian Journal of Chemistry. 2017. Vol. 5, no. 2. P. 144—151. DOI: 10.17721/fujcV5I2P144-151 (date of access: 25.07.2026).
Previously, phosphonic acid derivatives of calix[4]arene and thiacalix[4]arene were found to be potential inhibitors of protein tyrosine phosphatase 1B. In the present paper, the inhibitory activity of unsubstituted sulfonyl-bridget calix[4]arene towards some of the therapeutically important protein tyrosine phosphatases has been established. The obtained results showed that the sulfonylcalix[4]arene is able to inhibit protein tyrosine phosphatase MEG2 with IC50 value in the micromolar range. At the same time, the inhibitor demonstrated lower activity in case of other protein tyrosine phosphatases such as PTP1B, MEG1, TC-PTP, SHP2, and PTPβ. The performed molecular docking indicated that the inhibitor binds to the active site region of MEG2 and PTP1B with WPD-loop in the open conformation.
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