Stereo-specific Lasofoxifene Derivatives Reveal the Interplay between Estrogen Receptor Alpha Stability and Antagonistic Activity in ESR1 Mutant Breast Cancer Cells
D. J. Hosfield, S. Weber, N.-S. Li, M. Suavage, E. Sullivan, E. Nduwke, R. Han, S. Cush, M. Laine, S. C. Mader, G. L. Greene, S. W. Fanning
The paper synthesizes lasofoxifene derivatives to study how ER cellular lifetime and antagonistic activity relate in ESR1 mutant breast cancer cells, finding that reducing ER lifetime does not always enhance transcriptional antagonism.
bioRxiv · Aug 27, 2021Cancer Biology