Table 3.
Natural and synthetic ligands of nuclear receptors with circadian function.
| Nuclear receptors | Natural ligands | Synthetic ligands | References |
|---|---|---|---|
| LXR |
Oxysterols: 24(S)-hydroxycholesterol (brain) 22(R)-hydroxycholesterol (adrenal) 24(S),25-epoxycholesterol (liver) 27-hydroxycholesterol (human macrophage) Phytosterols: Stigmasterolsitosterolcampesterol |
T0901317 GW3965 |
[205], [207], [208] |
| LXRα | Intermediary cholesterol biosynthesis: 4,4-dimethyl-5a-cholesta-8,14,24-trien-3b-ol | [208] | |
| RXR | 9-cis retinoic Docosahexaenoic acid Phytanic acid |
Bexarotene PNCR |
[204], [205], [210] |
| RAR | Vitamin A and derivates All-trans-Retinoic acid (ATRA) |
Arotinoid acid Am 580 BMS209641 CD666 BMS270394 BMS204493 AGN193109 BMS195614 Ro-41-5253 PNCR |
[204], [210] |
| PPARα | Docosahexaenoic acid Eicosapentaenoic acid Leukotriene B4 8-hydroxy-eicosatetraenoic acid |
Fenofibrate Clofibrate Gemfibrozil |
[211] |
| PPARγ | Docosahexaenoic acid Eicosapentaenoic acid MUFA Arachidonic acid metabolites Triterpenoids |
thiazolidinediones | |
| PPARβ/δ | Long-chain fatty acids Carboprostacyclin Components of VLDL |
GW501516 | |
| RORα | Cholesterol Cholesterolsulphate 7α-hydroxycholesterol 7β-hydroxycholesterol 7-ketocholesterol 20α-hydroxycholesterol 22R-hydroxycholesterol 25-hydroxycholesterol 24S-hydroxycholesterol 24R-hydroxycholesterol 24,25-epoxycholesterol Neoruscogenin (25S)-ruscogenin |
T0901317 SR1078 SR3335 SR1001 |
[203] |
| RORγ | 7α-hydroxycholesterol 7β-hydroxycholesterol 7-ketocholesterol 24S-hydroxycholesterol 24R-hydroxycholesterol 24,25-epoxycholesterol |
T0901317 SR1078 SR2211 SR1555 SR1001 Digoxin Ursolic acid ML209 N-(4,6-dimethyl-benzo[d]thiazol-2-yl)-3-methyl-thiophene-2-carboxamide N-(2-(4-ethyl-phenyl)-2H-benzo-[d][1,2,3]triazol-5-yl) propionamide N-(5-benzoyl-4-p henylthiazol-2-yl)-2-(4-(ethylsulfonyl) phenyl)acetamide |
|
| RORβ | Stearic acid ATRA |
||
| NURR1 | In NURSA there are not ligands | 6-mercaptopurine Isoxazolopyridinone |
[212], [213] |
| TRα | Thyroid hormone | PNRC GC-1 |
[210] NURSA |
| ERRα | XCT790 Octochorocamphene |
NURSA | |
| SIRT6 (and other sirtuins) | Myristic, oleic and linoleic acids | [145] |