2019
DOI: 10.1158/1538-7445.am2019-922
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Abstract 922: Preclinical anticancer activity of LSZ102, a novel oral selective estrogen receptor degrader targeting wild-type and mutant ER

Abstract: Estrogen receptor (ER) blockade is a well-established therapeutic approach in ER+ breast cancer. A novel oral selective estrogen receptor degrader (SERD), LSZ102, is in development. LSZ102 induces proteasome-mediated degradation of both wild type and mutant ERα in MCF-7 cells. LSZ102 also inhibits transcription of ERα target genes and results in a decrease in cell proliferation in a dose dependent manner. Expression of ERα Y537S results in a shift in inhibition of cell proliferation upon incubation with either… Show more

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