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@article{1851239,
author = {Antonyová, Veronika and Kejík, Zdeněk and Brogyanyi, Tereza and Kaplánek, Robert and Veselá, Kateřina and Abramenko, Nikita and Ocelka, Tomáš and Masařík, Michal and Matkowski, Adam and Gburek, Jakub and Abel, Renata and Goede, Andrean and Preissner, Robert and Novotný, Petr and Jakubek, Milan},
article_location = {San Dieo},
article_number = {July 2022},
doi = {http://dx.doi.org/10.1016/j.bioorg.2022.105793},
keywords = {Cannabinoids; TET1 protein; Iron chelation; DNA methylation; Epigenetic},
language = {eng},
issn = {0045-2068},
journal = {Bioorganic Chemistry},
title = {Non-psychotropic cannabinoids as inhibitors of TET1 protein},
url = {https://www.sciencedirect.com/science/article/pii/S0045206822001985},
volume = {124},
year = {2022}
}
TY - JOUR
ID - 1851239
AU - Antonyová, Veronika - Kejík, Zdeněk - Brogyanyi, Tereza - Kaplánek, Robert - Veselá, Kateřina - Abramenko, Nikita - Ocelka, Tomáš - Masařík, Michal - Matkowski, Adam - Gburek, Jakub - Abel, Renata - Goede, Andrean - Preissner, Robert - Novotný, Petr - Jakubek, Milan
PY - 2022
TI - Non-psychotropic cannabinoids as inhibitors of TET1 protein
JF - Bioorganic Chemistry
VL - 124
IS - July 2022
SP - 1-8
EP - 1-8
PB - ACADEMIC PRESS INC ELSEVIER SCIENCE
SN - 00452068
KW - Cannabinoids
KW - TET1 protein
KW - Iron chelation
KW - DNA methylation
KW - Epigenetic
UR - https://www.sciencedirect.com/science/article/pii/S0045206822001985
N2 - Non-psychotropic cannabinoids (e.g., cannabidiol, cannabinol and cannabigerol) are contained in numerous alimentary and medicinal products. Therefore, predicting and studying their possible side effects, such as changes in DNA methylation, is an important task for assessing the safety of these products. Interference with TET enzymes by chelating ferrous ions can contribute to the altered methylation pattern. All tested cannabinoids displayed a strong affinity for Fe(II) ions. Cannabidiol and cannabinol exhibited potent inhibitory activities (IC50 = 4.8 and 6.27 μM, respectively) towards the TET1 protein, whereas cannabigerol had no effect on the enzyme activity. An in silico molecular docking study revealed marked binding potential within the catalytic cavity for CBD/CBN, but some affinity was also found for CBG, thus the total lack of activity remains unexplained. These results imply that cannabinoids could affect the activity of the TET1 protein not only due to their affinity for Fe(II) but also due to other types of interactions (e.g., hydrophobic interactions and hydrogen bonding).
ER -
ANTONYOVÁ, Veronika, Zdeněk KEJÍK, Tereza BROGYANYI, Robert KAPLÁNEK, Kateřina VESELÁ, Nikita ABRAMENKO, Tomáš OCELKA, Michal MASAŘÍK, Adam MATKOWSKI, Jakub GBUREK, Renata ABEL, Andrean GOEDE, Robert PREISSNER, Petr NOVOTNÝ and Milan JAKUBEK. Non-psychotropic cannabinoids as inhibitors of TET1 protein. \textit{Bioorganic Chemistry}. San Dieo: ACADEMIC PRESS INC ELSEVIER SCIENCE, 2022, vol.~124, July 2022, p.~1-8. ISSN~0045-2068. Available from: https://dx.doi.org/10.1016/j.bioorg.2022.105793.
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