Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

Somatic mutations in the estrogen receptor alpha (ERα) gene (ESR1), especially Y537S and D538G, have been linked to acquired resistance to endocrine therapies. Cell-based studies demonstrated that these mutants confer ERα constitutive activity and antiestrogen resistance and suggest that ligand-bind...

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Bibliographic Details
Main Authors: Sean W Fanning, Christopher G Mayne, Venkatasubramanian Dharmarajan, Kathryn E Carlson, Teresa A Martin, Scott J Novick, Weiyi Toy, Bradley Green, Srinivas Panchamukhi, Benita S Katzenellenbogen, Emad Tajkhorshid, Patrick R Griffin, Yang Shen, Sarat Chandarlapaty, John A Katzenellenbogen, Geoffrey L Greene
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2016-02-01
Series:eLife
Subjects:
breast cancer
acquired drug resistance
somatic mutation
estrogen receptor alpha
hormone
selective estrogen receptor modulators
Online Access:https://elifesciences.org/articles/12792

Internet

https://elifesciences.org/articles/12792

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