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

CSLog in Log in (EduId)

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.

Basic information

Original name

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

Authors

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

Edition

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

Other information

Language

English

Type of outcome

Article in a journal

Country of publisher

Germany

Confidentiality degree

is not subject to a state or trade secret

References:

URL

Organization

Lékařská fakulta – Repository – Repository

DOI

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

UT WoS

001158746700029

EID Scopus

2-s2.0-85184437842

Keywords in English

estrogen receptor modulators; immune checkpoint molecules

Links

LM2023053, research and development project. LX22NPO5102, research and development project. LX22NPO5107, research and development project. NU21-08-00407, research and development project.

Changed: 6/6/2024 04:52, RNDr. Daniel Jakubík

Abstract

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.

Files attached

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

Cite

ABRAMENKO, Nikita, Frederic VELLIEUX, Katerina VESELA, Zdenek KEJIK, Jan HAJDUCH, Michal MASAŘÍK, Petr BABULA, David HOSKOVEC, Karel PACAK, Pavel MARTASEK, Karel SMETANA and Milan JAKUBEK. Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules. Scientific Reports. London: Nature Publishing Group, 2024, vol. 14, No 1, p. 1-14. ISSN 2045-2322. Available from: 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 and Milan JAKUBEK. Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules. \textit{Scientific Reports}. London: Nature Publishing Group, 2024, vol.~14, No~1, p.~1-14. ISSN~2045-2322. Available from: https://dx.doi.org/10.1038/s41598-024-51804-2.