Discovering Small??Molecule Estrogen Receptor α/Coactivator Binding Inhibitors: High??Throughput Screening, Ligand Development, and Models for Enhanced …

…, Y Du, H Fu, JP Snyder, JA Katzenellenbogen

Index: Sun, Aiming; Moore, Terry W.; Gunther, Jillian R.; Kim, Mi-Sun; Rhoden, Eric; Du, Yuhong; Fu, Haian; Snyder, James P.; Katzenellenbogen, John A. ChemMedChem, 2011 , vol. 6, # 4 p. 654 - 666

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Citation Number: 21

Abstract

Abstract Small molecules, namely coactivator binding inhibitors (CBIs), that block estrogen signaling by directly inhibiting the interaction of the estrogen receptor (ER) with coactivator proteins act in a fundamentally different way to traditional antagonists, which displace the endogenous ligand estradiol. To complement our prior efforts at CBI discovery by de novo design, we used high-throughput screening (HTS) to identify CBIs of novel structure and ...