Table 1.
PPAR-γ ligands
| Ligand | Activity | Biological Activity | Ref |
|---|---|---|---|
| 15d-PGJ2 | agonist | In murine sepsis model, administration of ligand reduced lung injury and PMN trafficking to lung and intestine, blocked expression of adhesion molecules, and improved survival |
176 |
| Blocks inflammatory signaling through NF-κB, AP- 1, and STAT-1, thus reducing expression of Nos2, Mmp9, and Msr1 |
18, 19 |
||
| Covalently interacts with PPARγ LBD at Cys285 | 168 | ||
| Inhibits NF-κB activation by preventing degradation of IkBα in a PPAR-γ independent fashion |
174 | ||
| Inhibits MMP9 activity in human monocytes | 216 | ||
| 13-HODE | agonist | Decreases Nos2 expression in macrophages | 197 |
| Decreases CCR2 expression in THP1 human monocytes |
214 | ||
| Found in atherosclerotic plaques | 187 | ||
| 15-HETE | agonist | Decreases Nos2 expression in macrophages | 197 |
| Decreases superoxide production and degranulation of PMN stimulated by fMLP, LTB4, and PAF |
208 | ||
| Inhibits PMN migration across cytokine-activated endothelium in cell culture by reducing LTB4 receptors |
209, 210 |
||
| 9-HODE | agonist | Found in atherosclerotic plaques | 188 |
| Decreases CCR2 expression in THP1 human monocytes |
214 | ||
| Nitroalkene fatty acids |
Induce adipocyte differentiation and glucose uptake |
227, 228 |
|
| Block cytokine release and NF-κB activation in HUVECS stimulated by TNFα or atherogenic response |
231 | ||
| Decrease Nos2 and Mcp1 expression in RAW264.7 macrophages. Effect was not blocked by PPARγ synthetic antagonist |
232 | ||
| Covalently interact with PPARγ LBD in Cys285 at micromolar concentrations |
230 | ||
| 15-keto-PGE2 | agonist | Induces adipogenesis of 3T3L1 cells | 243 |
| Abundance of 15-keto-PGE2 was reduced in Cftr- null colonic epithelial cells, which exhibit defective PPAR-γ mediated gene expression |
112 | ||
| 5-methoxy-indole acetate |
agonist | serotonin metabolite that is bound to the AF-2 subpocket of PPAR-γ LBD. PPAR macrophage and stimulate 3T3-L1 adipogenesis. |
244 |
| PGF2a | antagonist | Inhibits adipocyte differentiation | 250 |
| Inhibits PPAR-γ activity by inducing phosphorylation of PPAR-γ at serine 112 |
250 | ||
| PPAR-γS112A knock-in mice maintained insulin sensitivity in model of diet-induced obesity |
251 | ||
| Cyclic phosphatidic acid |
antagonist | Stabilizes PPAR-γ-SMRT interaction | 252 |
| Blocks TZD-stimulated adipogenesis and lipid accumulation in macrophages |
|||
| Production induced by insulin, PMA, LPS, or H2O2 |