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DeMichele, A., Troxel, A.B., Berlin, J. A., Weber, A.L., Bunin, G.R., Turzo, E., Schinnar, R., Burgh, D., Berlin, M., Rubin, S.C., Rebbeck, T.R. and Strom, B.L. (2008) Impact of raloxifene or tamoxifen use on endometrial cancer risk: A population-based case-control study. Journal of Clinical Oncology, 26, 4151-4159. doi:10.1200/JCO.2007.14.0921

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• TITLE: More Stable, More Estrogenic: The SERM-ERα LBD Complex

  AUTHORS: Li Gao, Yaoquan Tu, Leif A. Eriksson

  KEYWORDS: Breast Cancer; Tamoxifen Resistance; Molecular Dynamics Simulations; Dihydrobenzoxathiin; SERM

  JOURNAL NAME: Journal of Biophysical Chemistry, Vol.2 No.3, August 9, 2011

  ABSTRACT: Many synthetic selective estrogen receptor modulators (SERMs) have been cocrystallized with the human estrogen receptor α ligand binding domain (ERα LBD). Despite stabilizing the same canonical inactive conformation of the LBD, most SERMs display different ligand-dependent pharmacological profiles. We show here that increased partial agonism of SERMs is associated with increased conformational stability of the SERM-LBD complexes, by investigation of dihydrobenzoxathiin-based SERMs using molecular modelling techniques. Analyses of tamoxifen (TAM) and 4-hydroxytamoxifen (OHT) in complex with the LBD furthermore indicates that the conversion of TAM to OHT increases both the affinity to ERα and the partial agonism of the anti-cancer drug, which provides a plausible explanation of the counterintuitive results of TAM therapy.