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
Structural and Molecular Mechanisms of Cytokine-Mediated Endocrine Resistance in Human Breast Cancer Cells.
Molecular Cell
Stender, Joshua D JD; Nwachukwu, Jerome C JC; Kastrati, Irida I; Kim, Yohan Y; Strid, Tobias T; Yakir, Maayan M; Srinivasan, Sathish S; Nowak, Jason J; Izard, Tina T; Rangarajan, Erumbi S ES; Carlson, Kathryn E KE; Katzenellenbogen, John A JA; Yao, Xin-Qiu XQ; Grant, Barry J BJ; Leong, Hon S HS; Lin, Chin-Yo CY; Frasor, Jonna J; Nettles, Kendall W KW; Glass, Christopher K CK