Article
The estrogen receptor alpha nuclear localization sequence is critical for fulvestrant-induced degradation of the receptor.
Molecular and cellular endocrinology - 5 Nov 2015
Casa Angelo J, Hochbaum Daniel, Sreekumar Sreeja, Oesterreich Steffi, Lee Adrian V
Abstract excerpt
Fulvestrant, a selective estrogen receptor down-regulator (SERD) is a pure competitive antagonist of estrogen receptor alpha (ERα). Fulvestrant binds ERα and reduces the receptor's half-life by increasing protein turnover, however, its mechanism of action is not fully understood. In this study, we show that removal of the ERα nuclear localization sequence (ERΔNLS) resulted in a predominantly cytoplasmic ERα that...
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