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Updated: Jun 27, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Tethered indoles as functionalizable ligands for the estrogen receptor
Bridget G Trogden1, Sung Hoon Kim, Shuyi Lee
1Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.
Abstract:
To create ligands for the estrogen receptor that contain pendant groups for tethering to a poly(amido)amine (PAMAM) dendrimer, we have explored a class of N-substituted 2-phenyl indoles. Attachment of tethers of different length and chemical nature to this non-steroidal indole scaffold gave high affinity ligand-tether conjugates that can be easily functionalized. To further explore the utility of this system, an indole-conjugated dendrimer was prepared and evaluated as an estrogen receptor ligand.
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