CAR, driving into the future.
CAR, driving into the future.
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DOI：
10.1210/me.2003-0397
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发表时间：
2004-07
影响因子：
--
通讯作者：
K. Swales;M. Negishi
中科院分区：
文献类型：
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作者：
K. Swales;M. Negishi
核孤儿受体 CAR 在没有配体的情况下具有活性，具有被激活剂进一步调节的独特能力。许多这些激活剂，包括苯巴比妥，不直接与受体结合。 CAR被认为是一种异生物质传感受体，响应这些化合物和其他细胞代谢物，转录修饰参与异生物质和类固醇代谢和消除的基因的表达。其肝脏表达模式赋予肝脏不仅能够抵御外源性损伤，还能够抵御内源性损伤的能力。 CAR 激活的机制很复杂，涉及在激活剂存在的情况下从细胞质易位到细胞核，然后在细胞核中进行进一步的激活步骤。尽管这一机制仍在研究中，但我们在此总结了迄今为止阐明的细胞信号通路，并推测了 CAR 激活剂通过该网络调节基因表达的机制。
The nuclear orphan receptor CAR is active in the absence of ligand with the unique capability to be further regulated by activators. A number of these activators, including phenobarbital, do not directly bind to the receptor. Considered a xenobiotic sensing receptor, CAR transcriptionally modifies the expression of genes involved in the metabolism and elimination of xenobiotics and steroids in response to these compounds and other cellular metabolites. Its hepatic expression pattern endows the liver with the ability to protect against not only exogenous but also endogenous insults. The mechanism of CAR activation is complex, involving translocation from the cytoplasm to the nucleus in the presence of activators, followed by further activation steps in the nucleus. Although this mechanism remains under investigation, we have summarized here the cellular signaling pathways elucidated so far and speculate on the mechanism by which CAR activators regulate gene expression through this network.