Nikita Abramenko, Fréderic Vellieux, Kateřina Veselá, Zdeněk Kejík, Jan Hajduch, Michal Masařík, Petr Babula, David Hoskovec, Karel Pacák, Pavel Martásek, Karel Smetana, Milan Jakubek
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...
February 6, 2024: Scientific Reports