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. Author manuscript; available in PMC: 2010 Sep 16.
Published in final edited form as: Nat Struct Mol Biol. 2008 Sep;15(9):924–931. doi: 10.1038/nsmb.1474

Figure 6. Cys285 is essential for the activity of covalent ligands.

Figure 6

Cell-based transcriptional activation assay using wild type and Cys285 mutants of PPARγ with 4-oxoDHA and 4HDHA. The three panels show the activation of a luciferase reporter gene by a Gal4 DBD- PPARγ LBD hybrid. The 4-oxoDHA is more active than 4-HDHA with the wild type receptor. Both the cysteine mutations impair the activity of the receptor. However it is clear that the activity of 4-oxoDHA is impaired more than that of 4-HDHA supporting the importance of covalent interactions in receptor activation.