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Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.

Nat Commun. 2018; 
Fanning S W,Hodges-Gallagher L,Myles D C,Sun R,Fowler C E,Plant I N,Green B D,Harmon C L,Greene G L,Kushner
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Mutagenesis Services .... by GenScript. Based on ERα LBD x- ray crystal structures, Q5 site-directed mutagenesis (New England Biolabs.... (residues 300-550) was synthesized by GenScript containing C381S, C417S, C530S, and L536S mutations in pET21 Get A Quote

摘要

Complex tissue-specific and cell-specific signaling by the estrogen receptor (ER) frequently leads to the development of resistance to endocrine therapy for breast cancer. Pure ER antagonists, which completely lack tissue-specific agonist activity, hold promise for preventing and treating endocrine resistance, however an absence of structural information hinders the development of novel candidates. Here we synthesize a small panel of benzopyrans with variable side chains to identify pure antiestrogens in a uterotrophic assay. We identify OP-1074 as a pure antiestrogen and a selective ER degrader (PA-SERD) that is efficacious in shrinking tumors in a tamoxifen-resistant xenograft model. Biochemical and cry... More

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