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- W2550923035 endingPage "118" @default.
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- W2550923035 abstract "Resistance to endocrine therapies remains a major clinical problem for the treatment of estrogen receptor-α (ERα)-positive breast cancer. On-target side effects limit therapeutic compliance and use for chemoprevention, highlighting an unmet need for new therapies. Here we present a full-antagonist ligand series lacking the prototypical ligand side chain that has been universally used to engender antagonism of ERα through poorly understood structural mechanisms. A series of crystal structures and phenotypic assays reveal a structure-based design strategy with separate design elements for antagonism and degradation of the receptor, and access to a structurally distinct space for further improvements in ligand design. Understanding structural rules that guide ligands to produce diverse ERα-mediated phenotypes has broad implications for the treatment of breast cancer and other estrogen-sensitive aspects of human health including bone homeostasis, energy metabolism, and autoimmunity." @default.
- W2550923035 created "2016-11-30" @default.
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- W2550923035 date "2016-11-21" @default.
- W2550923035 modified "2023-10-16" @default.
- W2550923035 title "Full antagonism of the estrogen receptor without a prototypical ligand side chain" @default.
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- W2550923035 doi "https://doi.org/10.1038/nchembio.2236" @default.
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