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Author response by David J Hosfield; Sandra Weber; Nan-Sheng Li; Madline Sauvage; Carstyn F Joiner; Govinda R Hancock; Emily A Sullivan; Estelle Ndukwe; Ross Han; Sydney Cush; Muriel Lainé; Sylvie C Mader; Geoffrey L Greene; Sean W Fanning is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Author response about?

Chemical manipulation of estrogen receptor alpha ligand binding domain structural mobility tunes receptor lifetime and influences breast cancer therapeutic activities. Selective estrogen receptor modulators (SERMs) extend estrogen receptor alpha (ERα) cellular lifetime/accumulation. They are antagonists in the breast but agonists in the uterine epithelium and/or in bone. Selective estrogen receptor degraders/downregulators (SERDs) reduce ERα cellular lifetime/accumulation and are pure antagonists. Activating somatic __ESR1__ mutations Y537S and D538G enable resistance to first-line endocrine therapies. SERDs have shown significant activities in __ESR1__ mutant setting while few SERMs have been studied. To understand whether chemical manipulation of ERα cellular lifetime and accumulation influences antagonistic activity, we studied a series of methylpyrollidine lasofoxifene (Laso) derivatives that maintained the drug’s antagonistic activities while uniquely tuning ERα cellular accumulation. These molecules were examined alongside a panel of antiestrogens in live cell assays of ERα cellular accumulation, lifetime, SUMOylation, and transcriptional antagonism. High-resolution x-ray cry

Who reads Author response?

Author

David J Hosfield; Sandra Weber; Nan-Sheng Li; Madline Sauvage; Carstyn F Joiner; Govinda R Hancock; Emily A Sullivan; Estelle Ndukwe; Ross Han; Sydney Cush; Muriel Lainé; Sylvie C Mader; Geoffrey L Greene; Sean W Fanning

Publisher

eLife Sciences Publications, Ltd

Published

2022

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)