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- W4286255065 abstract "Endocrine therapy is widely used in clinic for breast cancer treatment, but long-term treatment inevitably causes drug resistance. Most of endocrine therapy-resistant breast cancers continue to depend on ERα signaling for growth and survival. In this regard, small molecule-induced ERα degradation, i.e. proteolysis targeting chimeras (PROTACs), represents an effective strategy to overcome endocrine resistance. Herein, we describe the design, synthesis, and biological evaluation of novel ERα-targeting PROTACs, wherein a E3 ligase ligand was attached to the 11β-position of estradiol via various linkers. Our efforts have identified a potent ERα PROTAC 15b that achieved excellent ERα degradation activity (DC50 = 67 nM) and induced comparable inhibition of cell growth to that of fulvestrant in MCF-7 cells. Besides, 15b displayed antagonistic effects in uterine cells and favorable physicochemical properties, making it as a good lead compound for further development as anti-breast agents." @default.
- W4286255065 created "2022-07-21" @default.
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- W4286255065 date "2022-10-01" @default.
- W4286255065 modified "2023-09-29" @default.
- W4286255065 title "Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders" @default.
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- W4286255065 doi "https://doi.org/10.1016/j.jsbmb.2022.106154" @default.
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