The SERM/SERD Bazedoxifene Disrupts ESR1 Helix 12 to Overcome Acquired Hormone Resistance in Breast Cancer Cells
S. W. Fanning, R. Jeselsohn, V. Dharmarajan, C. G. Mayne, M. Karimi, G. Buchwalter, R. Houtman, W. Toy, C. E. Fowler, M. Laine, K. E. Carlson, T. A. Martin, J. Nowak, J. C. Nwachukwu, D. J. Hosfield, , G. L. Greene
This study shows that bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells by inhibiting Y537S and D538G ER mutants more effectively than tamoxifen.
bioRxiv · Apr 23, 2018Cancer Biology