Recent advances in peptidomimetics antagonists targeting estrogen receptor α-coactivator interaction in cancer therapy.
Bioorg Med Chem Lett
; 28(17): 2827-2836, 2018 09 15.
Article
em En
| MEDLINE
| ID: mdl-30025900
ABSTRACT
Estrogen receptor α (ERα) is a crucial target for ERα positive breast cancer treatment. Previous drug discovery efforts were focused on developing inhibitors that targeted the canonical ligand binding pockets of the ligand binding domain (LBD) of ERα. However, significant percentage of patients developed cancer relapse with drug-resistance. ERα peptidomimetic modulators have been considered as promising treatments for drug resistant breast cancers as they are targeting ERα-coactivator interacting interface instead of the ligand binding pocket of ERα. Herein, we reviewed the recent development of ERα peptidomimetics antagonists.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Alcaloides de Vinca
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Neoplasias da Mama
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Receptor alfa de Estrogênio
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Peptidomiméticos
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Antineoplásicos
Limite:
Animals
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Female
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Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article