Synthesis of a spin-labeled anti-estrogen as a dynamic motion probe for the estrogen receptor ligand binding domain |
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Authors: | Hendricks J Adam Gullà Stefano V Budil David E Hanson Robert N |
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Affiliation: | Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115-5000, United States. |
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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. |
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