Article
Classification of anti-estrogens according to intramolecular FRET effects on phospho-mutants of estrogen receptor alpha.
Molecular cancer therapeutics - 1 May 2007
Zwart Wilbert, Griekspoor Alexander, Rondaij Mariska, Verwoerd Desiree, Neefjes Jacques, Michalides Rob
Abstract excerpt
Anti-estrogen resistance is a major clinical problem in the treatment of breast cancer. In this study, fluorescence resonance energy transfer (FRET) analysis, a rapid and direct way to monitor conformational changes of estrogen receptor alpha (ERalpha) upon anti-estrogen binding, was used to characterize resistance to anti-estrogens. Nine different anti-estrogens all induced a rapid FRET response within minutes...
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