The DOI matches its Crossref record; 19 of the 19 references it cites were found in a registry or an index.
The Repressed Nuclear Receptor CAR Responds to Phenobarbital in Activating the Human CYP2B6 Gene
Open accessAbstract
The endogenous CYP2B6 gene becomes phenobarbital (PB) inducible in androstenol-treated HepG2 cells either transiently or stably transfected with a nuclear receptor CAR expression vector. The PB induction mediated by CAR is regulated by a conserved 51-base pair element called PB-responsive enhancer module (PBREM) that has now been located between -1733 and -1683 bp in the gene's 5'-flanking region. An in vitro translated CAR acting as a retinoid X receptor alpha heterodimer binds directly to the two nuclear receptor sites NR1 and NR2 within PBREM. In a stably transfected HepG2 cell line, both PBREM and NR1 are activated by PB and PB-type compounds such as chlorinated pesticides, polychlorinated biphenyls and chlorpromazine. In addition to PBREM, CAR also transactivates the steroid/rifampicin-response element of the human CYP3A4 gene in HepG2 cells. Thus, activation of the repressed nuclear receptor CAR appears to be a versatile mediator that regulates PB induction of the CYP2B and other genes.
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The nuclear receptor CAR mediates specific xenobiotic induction of drug metabolism
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Metadata
- Authors
- Sueyoshi, T., Kawamoto, T., Zelko, I., Honkakoski, P., & Negishi, M.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1999-03
- Volume
- 274
- Issue
- 10
- Pages
- 6043-6046
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1973238763
- Cited by
- 668
- References
- 19
- FWCI
- 39.10
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Sueyoshi, T., Kawamoto, T., Zelko, I., Honkakoski, P., & Negishi, M. (1999). The Repressed Nuclear Receptor CAR Responds to Phenobarbital in Activating the Human CYP2B6 Gene. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.274.10.6043
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