Title : Modulation of murine phenobarbital-inducible CYP2A5, CYP2B10 and CYP1A enzymes by inhibitors of protein kinases and phosphatases.

Pub. Date : 1999 Aug

PMID : 10447669






5 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Modulation of murine phenobarbital-inducible CYP2A5, CYP2B10 and CYP1A enzymes by inhibitors of protein kinases and phosphatases. Phenobarbital cytochrome P450, family 2, subfamily a, polypeptide 5 Mus musculus
2 In this study, the involvement of several protein kinase and phosphatase pathways on constitutive and phenobarbital-induced activities of CYP2A5, CYP2B10 and CYP1A1/2 in primary mouse hepatocytes was determined using well-defined chemical modulators of intracellular protein phosphorylation and desphosphorylation events. Phenobarbital cytochrome P450, family 2, subfamily a, polypeptide 5 Mus musculus
3 A 48-h treatment of the hepatocytes with 2-aminopurine, a nonspecific serine/threonine kinase inhibitor, elicited dose-dependent increases in both basal and phenobarbital-induced CYP2A5 catalytic activity (assayed as coumarin 7-hydroxylation), the maximal induction being 60-fold greater than the control value upon cotreatment with 1.5 mM phenobarbital and 10 mM 2-aminopurine. Phenobarbital cytochrome P450, family 2, subfamily a, polypeptide 5 Mus musculus
4 A 48-h treatment of the hepatocytes with 2-aminopurine, a nonspecific serine/threonine kinase inhibitor, elicited dose-dependent increases in both basal and phenobarbital-induced CYP2A5 catalytic activity (assayed as coumarin 7-hydroxylation), the maximal induction being 60-fold greater than the control value upon cotreatment with 1.5 mM phenobarbital and 10 mM 2-aminopurine. Phenobarbital cytochrome P450, family 2, subfamily a, polypeptide 5 Mus musculus
5 The serine/threonine phosphatase inhibitors tautomycin, calyculin A and okadaic acid all reduced both basal and phenobarbital-induced CYP2A5, CYP2B10 and CYP1A1/2 activities. Phenobarbital cytochrome P450, family 2, subfamily a, polypeptide 5 Mus musculus