Investigation of the potential effects of estrogen receptor
modulators on immune checkpoint molecules

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Investigation of the potential effects of estrogen receptor modulators on immune checkpoint ...

Přehled o publikaci

J 2024

Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules

ABRAMENKO, Nikita, Frederic VELLIEUX, Katerina VESELA, Zdenek KEJIK, Jan HAJDUCH et. al.

Základní údaje

Originální název

Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules

Autoři

ABRAMENKO, Nikita, Frederic VELLIEUX, Katerina VESELA, Zdenek KEJIK, Jan HAJDUCH, Michal MASAŘÍK, Petr BABULA, David HOSKOVEC, Karel PACAK, Pavel MARTASEK, Karel SMETANA a Milan JAKUBEK

Vydání

Scientific Reports, London, Nature Publishing Group, 2024, 2045-2322

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Stát vydavatele

Německo

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Organizace

Lékařská fakulta – Masarykova univerzita – Repozitář

DOI

http://dx.doi.org/10.1038/s41598-024-51804-2

UT WoS

001158746700029

EID Scopus

2-s2.0-85184437842

Klíčová slova anglicky

estrogen receptor modulators; immune checkpoint molecules

Návaznosti

LM2023053, projekt VaV. LX22NPO5102, projekt VaV. LX22NPO5107, projekt VaV. NU21-08-00407, projekt VaV.

Změněno: 6. 6. 2024 04:52, RNDr. Daniel Jakubík

Anotace

V originále

Immune checkpoints regulate the immune system response. Recent studies suggest that flavonoids, known as phytoestrogens, may inhibit the PD-1/PD-L1 axis. We explored the potential of estrogens and 17 Selective Estrogen Receptor Modulators (SERMs) as inhibiting ligands for immune checkpoint proteins (CTLA-4, PD-L1, PD-1, and CD80). Our docking studies revealed strong binding energy values for quinestrol, quercetin, and bazedoxifene, indicating their potential to inhibit PD-1 and CTLA-4. Quercetin and bazedoxifene, known to modulate EGFR and IL-6R alongside estrogen receptors, can influence the immune checkpoint functionality. We discuss the impact of SERMs on PD-1 and CTLA-4, suggesting that these SERMs could have therapeutic effects through immune checkpoint inhibition. This study highlights the potential of SERMs as inhibitory ligands for immune checkpoint proteins, emphasizing the importance of considering PD-1 and CTLA-4 inhibition when evaluating SERMs as therapeutic agents. Our findings open new avenues for cancer immunotherapy by exploring the interaction between various SERMs and immune checkpoint pathways.

Přiložené soubory

https://is.muni.cz/publication/2407998/Investigation_of_the_potential_effects_of_estrogen_receptor_modulators_on_immune_checkpoint_molecules.pdf

Citovat

ABRAMENKO, Nikita, Frederic VELLIEUX, Katerina VESELA, Zdenek KEJIK, Jan HAJDUCH, Michal MASAŘÍK, Petr BABULA, David HOSKOVEC, Karel PACAK, Pavel MARTASEK, Karel SMETANA a Milan JAKUBEK. Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules. Scientific Reports. London: Nature Publishing Group, 2024, roč. 14, č. 1, s. 1-14. ISSN 2045-2322. Dostupné z: https://dx.doi.org/10.1038/s41598-024-51804-2.

@article{61491,
   author = {Abramenko, Nikita and Vellieux, Frederic and Vesela, Katerina and Kejik, Zdenek and Hajduch, Jan and Masařík, Michal and Babula, Petr and Hoskovec, David and Pacak, Karel and Martasek, Pavel and Smetana, Karel and Jakubek, Milan},
   article_location = {London},
   article_number = {1},
   doi = {http://dx.doi.org/10.1038/s41598-024-51804-2},
   keywords = {estrogen receptor modulators; immune checkpoint molecules},
   language = {eng},
   issn = {2045-2322},
   journal = {Scientific Reports},
   title = {Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules},
   url = {https://www.nature.com/articles/s41598-024-51804-2},
   volume = {14},
   year = {2024}
}

TY  - JOUR
ID  - 61491
AU  - Abramenko, Nikita - Vellieux, Frederic - Vesela, Katerina - Kejik, Zdenek - Hajduch, Jan - Masařík, Michal - Babula, Petr - Hoskovec, David - Pacak, Karel - Martasek, Pavel - Smetana, Karel - Jakubek, Milan
PY  - 2024
TI  - Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules
JF  - Scientific Reports
VL  - 14
IS  - 1
SP  - 1-14
EP  - 1-14
PB  - Nature Publishing Group
SN  - 2045-2322
KW  - estrogen receptor modulators
KW  - immune checkpoint molecules
UR  - https://www.nature.com/articles/s41598-024-51804-2
N2  - Immune checkpoints regulate the immune system response. Recent studies suggest that flavonoids, known as phytoestrogens, may inhibit the PD-1/PD-L1 axis. We explored the potential of estrogens and 17 Selective Estrogen Receptor Modulators (SERMs) as inhibiting ligands for immune checkpoint proteins (CTLA-4, PD-L1, PD-1, and CD80). Our docking studies revealed strong binding energy values for quinestrol, quercetin, and bazedoxifene, indicating their potential to inhibit PD-1 and CTLA-4. Quercetin and bazedoxifene, known to modulate EGFR and IL-6R alongside estrogen receptors, can influence the immune checkpoint functionality. We discuss the impact of SERMs on PD-1 and CTLA-4, suggesting that these SERMs could have therapeutic effects through immune checkpoint inhibition. This study highlights the potential of SERMs as inhibitory ligands for immune checkpoint proteins, emphasizing the importance of considering PD-1 and CTLA-4 inhibition when evaluating SERMs as therapeutic agents. Our findings open new avenues for cancer immunotherapy by exploring the interaction between various SERMs and immune checkpoint pathways.
ER  -

ABRAMENKO, Nikita, Frederic VELLIEUX, Katerina VESELA, Zdenek KEJIK, Jan HAJDUCH, Michal MASAŘÍK, Petr BABULA, David HOSKOVEC, Karel PACAK, Pavel MARTASEK, Karel SMETANA a Milan JAKUBEK. Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules. \textit{Scientific Reports}. London: Nature Publishing Group, 2024, roč.~14, č.~1, s.~1-14. ISSN~2045-2322. Dostupné z: https://dx.doi.org/10.1038/s41598-024-51804-2.