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Defining the Communication Between Agonist and Coactivator Binding in the Retinoid X Receptor a Ligand Binding Domain

Published: Wednesday, November 06, 2013
Last Updated: Wednesday, November 06, 2013
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The four structural changes are conserved in all x-ray structures of the RXR ligand binding domain in the presence of agonist and coactivator peptide.

Background: Some retinoid X receptor (RXR)  agonists have potential as cancer drugs.

Results: Structures of RXR in complex with two  different agonists show similar folds. Dynamics  analysis reveals unique ligand-induced dynamics  in helices 3, 11, and 12.

Conclusion: Two networks of interactions which  connect RXR agonists to coactivator binding are  defined.

Significance: Recognizing common  conformational changes and distinguishing  dynamics of RXR-selective agonists is needed for  advances in drug design.

This article was published online in The Journal of Biological Chemistry and is free to access.


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