Identification of Bexarotene as a PPAR Antagonist with HDX

Figure 1

Differential HDX of PPARγ:RXRα heterodimer with Bexarotene: (a) residues colored corresponding to the average percent change in deuteration between apo and Bexarotene bound complex over 6 time points (10, 30, 60, 300, 900, and 3600 seconds) run in triplicate () overlaid on PDB:1 K74. HDX buildup curves of (b) RXRα helix 10/11 peptide (RSIGLKC) at the dimer interface, (c) RXRα peptide (SHRSIAVKDGIL) containing arginine 316 known to form a hydrogen bond with Bexarotene in crystal structure PDB 4K61, and (d) PPARγ LBD helix 11 peptide (RQIVTEHVQL) at dimer interface.

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