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.

• MeSH
• antigen CTLA-4 MeSH
• antigeny CD274 MeSH
• antigeny CD279 MeSH
• imunoterapie MeSH
• lidé MeSH
• modulátory estrogenních receptorů MeSH
• nádory * terapie   MeSH
• proteiny kontrolních bodů imunitní reakce * MeSH
• quercetin MeSH
• selektivní modulátory estrogenních receptorů farmakologie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antigen CTLA-4 MeSH
• antigeny CD274 MeSH
• antigeny CD279 MeSH
• modulátory estrogenních receptorů MeSH
• proteiny kontrolních bodů imunitní reakce * MeSH
• quercetin MeSH
• selektivní modulátory estrogenních receptorů MeSH