Products/Services Used | Details | Operation |
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Stable Cell Line Development Services> | The PiggyBac transposon system was used to enable stable expression of either wild-type or mutant ER, tagged at its N terminus with mNeon (GenScript), in MCF7 cells. | Get A Quote |
Estrogen receptor-positive (ER) breast cancers frequently remain dependent on ER signaling even after acquiring resistance to endocrine agents, prompting the development of optimized ER antagonists. Fulvestrant is unique among approved ER therapeutics due to its capacity for full ER antagonism, thought to be achieved through ER degradation. The clinical potential of fulvestrant is limited by poor physicochemical features, spurring attempts to generate ER degraders with improved drug-like properties. We show that optimization of ER degradation does not guarantee full ER antagonism in breast cancer cells; ER "degraders" exhibit a spectrum of transcriptional activities and anti-proliferative potential. Mecha... More