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.
