The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux

@article{Synold2001TheON,
  title={The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux},
  author={Timothy W. Synold and Isabelle Dussault and Barry Marc Forman},
  journal={Nature Medicine},
  year={2001},
  volume={7},
  pages={584-590}
}
Cytochrome P450 3A4 is an important mediator of drug catabolism that can be regulated by the steroid and xenobiotic receptor (SXR). We show here that SXR also regulates drug efflux by activating expression of the gene MDR1, which encodes the protein P-glycoprotein (ABCB1). Paclitaxel (Taxol), a commonly used chemotherapeutic agent, activated SXR and enhanced P-glycoprotein–mediated drug clearance. In contrast, docetaxel (Taxotere), a closely related antineoplastic agent, did not activate SXR… CONTINUE READING
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