Title: Selectively targeting estrogen receptors for cancer treatment.

Authors: Shanle, Erin K; Xu, Wei

Published In Adv Drug Deliv Rev, (2010 Oct 30)

Abstract: Estrogens regulate growth and development through the action of two distinct estrogen receptors (ERs), ERýý and ERýý, which mediate proliferation and differentiation of cells. For decades, ERýý 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 ERýý going beyond ligand-dependent activity are under current investigation. As evidence of the anti-proliferative role of ERýý accumulates, selectively targeting ERýý 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 ERýý and ERýý for cancer treatment.

PubMed ID: 20708050

MeSH Terms: No MeSH terms associated with this publication