Synthesis of a spin-labeled anti-estrogen as a dynamic motion probe for the estrogen receptor ligand binding domain
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 conform...
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Published in | Bioorganic & medicinal chemistry letters Vol. 22; no. 4; pp. 1743 - 1746 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
Amsterdam
Elsevier Ltd
15.02.2012
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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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Bibliography: | http://dx.doi.org/10.1016/j.bmcl.2011.12.091 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 ObjectType-Article-2 ObjectType-Feature-1 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2011.12.091 |