Table 1.
NRs associated with metabolic disease, and their synthetic ligands. Refer to text for details.
| Receptor (or coactivator) | Associated Metabolic Disease or Pathologies | Synthetic ligand or modulator being used to ameliorate metabolic disease | Other representative synthetic ligands |
|---|---|---|---|
| GR | Viceral obesity, hyperglycemia | N/A | Dexamethasone, RU38486 |
| MR | Hypertension
Cardiac failure |
Aldosterone antagonist (Spironolactone, Eplerenone) | fludrocortisone |
| TRβ | Hypercholesterolemia | N/A | GC-1, KB-141 |
| PPARα | Dyslipidemia
Atherosclerosis |
fibrate (Gemfibrozil, fenofibrate, clofibrate) | WY14643 |
| PPARγ | Diabetes Mellitus, insulin-resistant
Atherosclerosis |
thiazolidinedione (pioglitazone, rosiglitazone) | FMOC-L-Leucine |
| PPARδ | Dyslipidemia
Atherosclerosis |
N/A | GW501516, KD3010 |
| LXRα/β | Dyslipidemia
Atherosclerosis |
N/A | T0901317, GW3965 |
| FXR | Hypercholesterolemia
Bilary cholestasis Dyslipidemia |
guggulsterone (antagonist) chenodeoxycholic acid (agonist) | Fexaramine, GW4046 |
| PXR | Bilary cholestasis, jaundice | St. John’s wort (hyperforin), rifampin | SR12813 |
| CAR | Bilary cholestasis, jaundice | Yin Zhi Huang (6,7-dimethylesculetin) | CITCO |
| ERRα/γ | Insulin resistance | N/A | XCT790, 4-hydroxytamoxifen |
| HNF4α | MODY, type I
Non-Insulin Dependent Diabetes Mellitus |
N/A | N/A |
| SHP | Mild obesity | N/A | N/A |
| RORα | Atherosclerosis | N/A | N/A |