Activation and Nuclear Translocation of CAR

Activation and nucleocytoplasmic translocation of CAR have been studied extensively. CAR is normally localized in the cytoplasm of liver cells. When treated with PB, CAR is translocated to the nucleus. This is the first step of activation of CAR in response to drug treatment. PB does not bind to the ligand binding domain (LBD) of human or mouse CAR. TCPOBOP binds mouse but not human CAR. In general, active transport of nuclear receptors from the cytoplasm to the nucleus requires a short sequence called the nuclear localization signal (NLS) that is exposed 

Nuclear Receptors in Drug Metabolism Edited by Wen Xie Copyright 2009 John Wiley Sons, Inc. 

---