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...

Full description

Bibliographic Details
Main Authors: Fanning, Sean W, Mayne, Christopher G, Dharmarajan, Venkatasubramanian, Carlson, Kathryn E, Martin, Teresa A, Novick, Scott J, Toy, Weiyi, Green, Bradley, Panchamukhi, Srinivas, Katzenellenbogen, Benita S, Tajkhorshid, Emad, Griffin, Patrick R, Shen, Yang, Chandarlapaty, Sarat, Katzenellenbogen, John A, Greene, Geoffrey L
Format: Online
Language:English
Published: eLife Sciences Publications, Ltd 2016
Online Access:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4821807/