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

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Authors

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

Year of publication 2024
Type Article in Periodical
Magazine / Source Nature Scientific Reports
MU Faculty or unit

Faculty of Medicine

Citation
Web https://www.nature.com/articles/s41598-024-51804-2
Doi http://dx.doi.org/10.1038/s41598-024-51804-2
Keywords estrogen receptor modulators; immune checkpoint molecules
Attached files
Description 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.
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