The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells

The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells

Acquired resistance to endocrine therapy remains a significant clinical burden for breast cancer patients. Somatic mutations in the ESR1 (estrogen receptor alpha (ERα)) gene ligand-binding domain (LBD) represent a recognized mechanism of acquired resistance. Antiestrogens with improved efficacy vers...

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Bibliographic Details
Main Authors: Sean W Fanning, Rinath Jeselsohn, Venkatasubramanian Dharmarajan, Christopher G Mayne, Mostafa Karimi, Gilles Buchwalter, René Houtman, Weiyi Toy, Colin E Fowler, Ross Han, Muriel Lainé, Kathryn E Carlson, Teresa A Martin, Jason Nowak, Jerome C Nwachukwu, David J Hosfield, Sarat Chandarlapaty, Emad Tajkhorshid, Kendall W Nettles, Patrick R Griffin, Yang Shen, John A Katzenellenbogen, Myles Brown, Geoffrey L Greene
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2018-11-01
Series:eLife
Subjects:
breast cancer
acquired drug resistance
hormone therapy
ESR1 Somatic Mutation
estrogen receptor
selective estrogen receptor Degrader
Online Access:https://elifesciences.org/articles/37161

Internet

https://elifesciences.org/articles/37161

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