Chapter title |
A structural explanation for ERalpha/ERbeta SERM discrimination.
|
---|---|
Chapter number | 3 |
Book title |
New Molecular Mechanisms of Estrogen Action and Their Impact on Future Perspectives in Estrogen Therapy
|
Published in |
Ernst Schering Research Foundation workshop, January 2004
|
DOI | 10.1007/978-3-662-05386-7_3 |
Pubmed ID | |
Book ISBNs |
978-3-66-205388-1, 978-3-66-205386-7
|
Authors |
G. L. Greene, A. K. Shiau, K. W. Nettles, Greene, G. L., Shiau, A. K., Nettles, K. W. |
Abstract |
Many NRs have multiple subtypes that possess distinct expression patterns and that regulate distinct target genes. Antagonists generated through the addition of bulky side chains to agonist scaffolds are limited to being antagonistic on one or more subtypes of a particular NR. The passive antagonism mechanism, as revealed in our studies through direct comparison of the two THC-ER LBD complexes, suggests a new approach to achieving NR antagonism. Compounds could be designed to selectively stabilize the inactive conformations of certain NR subtypes and the active conformations of others. Such ligands are likely to exert novel biological and therapeutic effects. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 1 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 1 | 100% |
Readers by discipline | Count | As % |
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Unknown | 1 | 100% |