Selectively targeting estrogen receptors for cancer treatment.
Adv Drug Deliv Rev
; 62(13): 1265-76, 2010 Oct 30.
Article
em En
| MEDLINE
| ID: mdl-20708050
ABSTRACT
Estrogens regulate growth and development through the action of two distinct estrogen receptors (ERs), ERα and ERß, which mediate proliferation and differentiation of cells. For decades, ERα 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 ERα going beyond ligand-dependent activity are under current investigation. As evidence of the anti-proliferative role of ERß accumulates, selectively targeting ERß 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 ERα and ERß for cancer treatment.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Moduladores Seletivos de Receptor Estrogênico
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Receptor alfa de Estrogênio
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Receptor beta de Estrogênio
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Terapia de Alvo Molecular
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Neoplasias
Limite:
Female
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Humans
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Male
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article