Nuclear translocation of adenoviral-enhanced yellow fluorescent protein-tagged-human constitutive androstane receptor (hCAR): a novel tool for screening hCAR activators in human primary hepatocytes.

ABSTRACT: The constitutive androstane receptor [(CAR) NR1I3] is a hepatic transcription factor that controls the expression of numerous drug-metabolizing enzymes and transporters in response to xenobiotic exposures. In primary hepatocytes and intact liver, CAR resides in the cytoplasm under basal condition and translocates to the nucleus upon exposure to inducers. However, CAR spontaneously accumulates in the nucleus of immortalized cell lines and exhibits constitutive activation in the absence of activators, which makes the identification of CAR activators extremely challenging. Here, we have established an efficient screening method for determining the nuclear translocation of human (h) CAR in human primary hepatocytes (HPHs). Our results demonstrated that adenoviral-enhanced yellow fluorescent pr

SUBMITTER: Li H 

PROVIDER: S-EPMC2683392 | biostudies-literature | 2009 May

REPOSITORIES: biostudies-literature