Inhibitors | Comment | Organism | Structure |
---|---|---|---|
N-benzoloxycarbonyl-Leu-Leu-leucinal | MG132, high concentrations are cytotoxic and can suppress CYP3A synthesis. Biphasic concentration effect on CYP3A turnover: stabilization at 0.005 to 0.01 mM with marked suppression at more than 0.1 mM. Marked (approximately 4fold) MG132 concentration-dependent RNA-dependent protein kinase-like ER-bound elF2alpha-kinase autophosphorylation, along with an 8fold increase in elF2alpha-phosphorylation. In parallel, MG132 also activates general control nonderepressible-2 elF2alpha kinase in a concentration-dependent manner, but not the heme-regulated inhibitor elF2alpha kinase. Consequently dramatic translational shutoff of total hepatic protein, including but not limited to CYP3A and tryptophan 2,3-dioxygenase protein syntheses | Rattus norvegicus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
endoplasmic reticulum | - |
Rattus norvegicus | 5783 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
male sprague-dawley rats | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
hepatocyte | - |
Rattus norvegicus | - |
Synonyms | Comment | Organism |
---|---|---|
CYP3A | - |
Rattus norvegicus |
cytochrome P450 3A | - |
Rattus norvegicus |
P450s 3A | - |
Rattus norvegicus |
Organism | Comment | Expression |
---|---|---|
Rattus norvegicus | dexamethasone-mediated CYP3A induction | up |