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. 1999 May 25;96(11):6102–6106. doi: 10.1073/pnas.96.11.6102

Figure 2.

Figure 2

GW0072 is a PPARγ ligand with a unique functional profile. (A) Dose response on the PPARγ-GAL4 chimera for GW0072 (○) and GW0072 plus 100 nM rosiglitazone (●). Reporter activity was expressed as the % of the maximal activation by 1 μM rosiglitazone. GW0072 demonstrates competitive antagonism of rosiglitazone but retains weak agonist activity at μM concentrations. (B) Activity on full-length PPARγ2 for 100 nM rosiglitazone (TZD), 10 μM GW0072 (GW), and 100 nM rosiglitazone plus 10 μM GW0072 (TZD + GW). Vehicle was 0.1% DMSO. Reporter activity was expressed as the % of the maximal activation by 1 μM rosiglitazone. (C–F) The functional activity of GW0072 is paralleled by its effects on coactivator recruitment to PPARγ2 in a mammalian two-hybrid assay. GW0072 (GW) (10 μM) antagonizes recruitment of the coactivators CBP and SRC1 promoted by 1 μM rosiglitazone (TZD). GW0072 (GW) (10 μM) does not recruit the corepressors NCoR or SMRT.