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

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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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