Article
Monitoring ligand-mediated helix 12 transitions within the human estrogen receptor α using bipartite tetracysteine display.
Organic & biomolecular chemistry - 21 Aug 2020
Pokhrel Ranju, Tang Tang, Holub Justin M
Abstract excerpt
Estrogen receptor α ligand-binding domains (ERα-LBD) expressing tetracysteine motifs bind FlAsH-EDT2 upon transition of helix 12 (H12) to a folded state. Changes in fluorescence intensity allowed surveillance of ligand-mediated H12 transitions and facilitated the determination of FlAsH association rates (kon) and apparent equilibrium dissociation constants (Kapp) to ERα-LBDs in the presence of estrogenic ligands.
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