Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.
Nature Communications
Fanning, S W SW; Hodges-Gallagher, L L; Myles, D C DC; Sun, R R; Fowler, C E CE; Plant, I N IN; Green, B D BD; Harmon, C L CL; Greene, G L GL; Kushner, P J PJ