Nonsteroidal bivalent estrogen ligands: an application of the bivalent concept to the estrogen receptor.

Abstract

The estrogen receptor (ER) is a hormone-regulated transcription factor that binds, as a dimer, to estrogens and to specific DNA sequences. To explore at a fundamental level the geometric and topological features of bivalent-ligand binding to the ER dimer, dimeric ER crystal structures were used to rationally design nonsteroidal bivalent estrogen ligands… (More)
DOI: 10.1021/cb3006243

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