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Selectively targeting estrogen receptors for cancer treatment Shanle EK; Xu WAdv Drug Deliv Rev 2010[Oct]; 62 (13): 1265-76Estrogens regulate growth and development through the action of two distinct estrogen receptors (ERs), ERalpha and ERbeta, which mediate proliferation and differentiation of cells. For decades, ERalpha mediated estrogen signaling has been therapeutically targeted to treat breast cancer, most notably with the selective estrogen receptor modulator (SERM) tamoxifen. Selectively targeting ERs occurs at two levels: tissue selectivity and receptor subtype selectivity. SERMs have been developed with emphasis on tissue selectivity to target ER signaling for breast cancer treatment. Additionally, new approaches to selectively target the action of ERalpha going beyond ligand-dependent activity are under current investigation. As evidence of the anti-proliferative role of ERbeta accumulates, selectively targeting ERbeta is an attractive approach for designing new cancer therapies with the emphasis shifted to designing ligands with subtype selectivity. This review will present the mechanistic and structural features of ERs that determine tissue and subtype selectivity with an emphasis on current approaches to selectively target ERalpha and ERbeta for cancer treatment.|*Molecular Targeted Therapy[MESH]|Breast Neoplasms/drug therapy/metabolism[MESH]|Estrogen Receptor alpha/chemistry/*metabolism[MESH]|Estrogen Receptor beta/chemistry/*metabolism[MESH]|Female[MESH]|Humans[MESH]|Ligands[MESH]|Male[MESH]|Molecular Conformation[MESH]|Neoplasms/*drug therapy/*metabolism[MESH]|Selective Estrogen Receptor Modulators/chemistry/*metabolism/*therapeutic use[MESH]|Signal Transduction[MESH]|Structure-Activity Relationship[MESH] |
