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Literature summary for 1.14.14.1 extracted from

  • Acharya, P.; Engel, J.C.; Correia, M.A.
    Hepatic CYP3A suppression by high concentrations of proteasomal inhibitors: a consequence of endoplasmic reticulum (ER) stress induction, activation of RNA-dependent protein kinase-like ER-bound eukaryotic initiation factor 2alpha (eIF2alpha)-kinase (PERK) (2009), Mol. Pharmacol., 76, 503-515.
    View publication on PubMedView publication on EuropePMC

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
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Rattus norvegicus 5783
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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male sprague-dawley rats
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Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
CYP3A
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Rattus norvegicus
cytochrome P450 3A
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Rattus norvegicus
P450s 3A
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Rattus norvegicus

Expression

Organism Comment Expression
Rattus norvegicus dexamethasone-mediated CYP3A induction up