Title : Ser100-Phosphorylated RORα Orchestrates CAR and HNF4α to Form Active Chromatin Complex in Response to Phenobarbital to Regulate Induction of CYP2B6.

Pub. Date : 2020 Mar

PMID : 31924695






5 Functional Relationships(s)
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Protein Name
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1 Ser100-Phosphorylated RORalpha Orchestrates CAR and HNF4alpha to Form Active Chromatin Complex in Response to Phenobarbital to Regulate Induction of CYP2B6. Phenobarbital cytochrome P450 family 2 subfamily B member 6 Homo sapiens
2 Here, we found serine 100-phosphorylated RORalpha orchestrates constitutive androstane receptor (CAR) and hepatocyte nuclear factor 4 alpha (HNF4alpha) to induce CYP2B6 by phenobarbital (PB) in human primary hepatocytes (HPHs). Phenobarbital cytochrome P450 family 2 subfamily B member 6 Homo sapiens
3 Here, we found serine 100-phosphorylated RORalpha orchestrates constitutive androstane receptor (CAR) and hepatocyte nuclear factor 4 alpha (HNF4alpha) to induce CYP2B6 by phenobarbital (PB) in human primary hepatocytes (HPHs). Phenobarbital cytochrome P450 family 2 subfamily B member 6 Homo sapiens
4 Altogether, the results established that p-Ser100 RORalpha bridging the PBREM and OARE orchestrates CAR and HNF4alpha to form active chromatin complex during PB-induced CYP2B6 expression in human primary hepatocytes. Phenobarbital cytochrome P450 family 2 subfamily B member 6 Homo sapiens
5 SIGNIFICANCE STATEMENT: CYP2B6 is a vital enzyme for the metabolic elimination of xenobiotics, and it is prone to induction by xenobiotics, including phenobarbital via constitutive androstane receptor (CAR) and hepatocyte nuclear factor 4 alpha (HNF4alpha). Phenobarbital cytochrome P450 family 2 subfamily B member 6 Homo sapiens