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- W3216037734 endingPage "74" @default.
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- W3216037734 abstract "Abstract The estrogen receptor (ER) has historically played and continues to play a prominent role in drug discovery as a target for medicinal chemists. The first targeted cancer therapy was directed at ERα and the first clinical drug that is a proteolysis targeting small molecule is also an ER ligand used to treat metastatic breast cancer. The last decade has been described as a renaissance in the medicinal chemistry of endocrine therapy, therefore, this article focuses on design of small molecule ERα ligands for treatment of hormone‐dependent breast cancer. As our understanding of the role of ER in resistance to endocrine therapy increases, further opportunities will be presented for medicinal chemists to design therapeutic agents for metastatic disease. Beyond breast cancer, ER, whether nuclear or extranuclear remains largely unexploited as a target for small molecule drug design, which is partly explained by the complexity of the underlying biology and partly by the cooling influence of the initial Women's Health Initiative outcomes on estrogen replacement therapy. Old and new concepts of ligand binding and signal transduction by ER are presented to stimulate the interests of medicinal chemists; accompanied by a catalogue of newer small molecule ligands reported in the literature and their interactions with ER." @default.
- W3216037734 created "2021-12-06" @default.
- W3216037734 creator A5009700001 @default.
- W3216037734 creator A5020757036 @default.
- W3216037734 creator A5035807724 @default.
- W3216037734 creator A5061807616 @default.
- W3216037734 date "2021-04-26" @default.
- W3216037734 modified "2023-10-16" @default.
- W3216037734 title "Estrogen Receptor Modulators" @default.
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