Toxicology: Drug Metabolism and Transport
Nuclear receptors included this assay panel influence drug metabolism and transport. Specific nuclear receptors are involved in drug-drug interactions via regulation of the cytochrome P450 family of enzymes. Screening of compounds against this panel facilitates the identification of toxicology problems early in the drug discovery process. Each receptor is linked to the NCBI database, Genecards, and Geneatlas. Some receptors are linked to additional pathway maps. Click on any object in a pathway for more detailed information.
| Receptors |
NCBI |
Genecards |
Geneatlas |
||
| CAR |
Constitutive androstane receptor |
N |
G |
GA |
|
| FXR |
Farnesoid X receptor |
N |
G |
GA |
|
| TRalpha |
Thyroid hormone receptor alpha |
N |
G |
GA |
|
| PPARalpha |
Peroxisome proliferator-activated receptor alpha |
N |
G |
GA |
|
| LXRbeta |
Liver X receptor beta |
N |
G |
GA |
References:
- Willson, T.M. and Kliewer, S.A. "PXR, CAR and Drug Metabolism" Nat. Rev. Drug Disc. 2002, 1, 259-266. Abstract.
- Kliewer, S.A.; Goodwin, B. and Willson, T.M. "The Nuclear Pregnane X Receptor: A Key Regulator of Xenobiotic Metabolism" Endo. Rev. 2002, 23, (5), 687-702. Abstract.
- Kretschmer, X.C. and Baldwin, W.S. "CAR and PXR: Xenosensors of Endocrine Disrupters?" Chem. Biol. Interact., 2005, 155, 111-128. Abstract.
- Dixit, S.G.; Tirona, R.G. and Kim, R.B. "Beyond CAR and PXR" Curr. Drug Metab. 2005, 6, (4), 385-97. Abstract.
Some useful nuclear receptor links:
The Nuclear Receptor Resource
PPAR Resource Page
Nuclear Receptor Signaling Atlas
