Article
The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor.
Molecular cancer therapeutics - 1 Jul 2020
Andreano Kaitlyn J, Baker Jennifer G, Park Sunghee, Safi Rachid, Artham Sandeep, Oesterreich Steffi, Jeselsohn Rinath, Brown Myles, Sammons Sarah, Wardell Suzanne E, Chang Ching-Yi, Norris John D, McDonnell Donald P
Abstract excerpt
The estrogen receptor (ER/ESR1) is expressed in a majority of breast cancers and drugs that inhibit ER signaling are the cornerstone of breast cancer pharmacotherapy. Currently, aromatase inhibitors are the frontline endocrine interventions of choice although their durability in metastatic disease is limited by activating point mutations within the ligand-binding domain of ESR1 that permit ligand-independent...
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