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Updated: May 25, 2026

11:19
Site Directed Spin Labeling and EPR Spectroscopic Studies of Pentameric Ligand-Gated Ion Channels
Published on: July 4, 2016
Synthesis of a spin-labeled anti-estrogen as a dynamic motion probe for the estrogen receptor ligand binding domain
J Adam Hendricks1, Stefano V Gullà, David E Budil
1Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115-5000, United States.
Bioorganic & Medicinal Chemistry Letters
|January 20, 2012
Abstract:
The preparation and characterization of a novel nitroxide spin probe based on a steroidal anti-estrogen is described. The probe 5 demonstrated very high binding affinity for both the alpha and beta isoforms of the estrogen receptor-ligand binding domain. EPR spectrometric studies demonstrate conformational constraints for the ligand, consistent with the nitroxyl moiety occupying a position just beyond the receptor-solvent interface.

