Title:Recent Advances in Hepatic Metabolic Regulation by the Nuclear Factor
Rev-erbɑ
Volume: 25
Issue: 1
Author(s): Qi Zhang, Yutong Chen, Jingqi Li, Haishan Xia, Yongbin Tong*Yuyu Liu*
Affiliation:
- College of Pharmacy, Guangdong Medical University, Dongguan, China
- College of Pharmacy, Guangdong Medical University, Dongguan, China
Keywords:
Rev-erbɑ, liver, xenobiotic metabolism, enzymes, obesity, drug metabolism enzymes, apolipoprotein A-IV.
Abstract: Rev-erbɑ (NR1D1) is a nuclear receptor superfamily member that plays a vital role in mammalian molecular clocks
and metabolism. Rev-erbɑ can regulate the metabolism of drugs and the body's glucose metabolism, lipid metabolism, and adipogenesis.
It is even one of the important regulatory factors regulating the occurrence of metabolic diseases (e.g., diabetes, fatty
liver). Metabolic enzymes mediate most drug metabolic reactions in the body. Rev-erbɑ has been recognized to regulate
drug metabolic enzymes (such as Cyp2b10 and Ugt1a9). Therefore, this paper mainly reviewed that Rev-erbɑ regulates I and
II metabolic enzymes in the liver to affect drug pharmacokinetics. The expression of these drug metabolic enzymes (up-regulated
or down-regulated) is related to drug exposure and effects/ toxicity. In addition, our discussion extends to Rev-erbɑ regulating
some transporters (such as P-gp, Mrp2, and Bcrp), as they also play an essential role in drug metabolism. Finally, we
briefly describe the role and mechanism of nuclear receptor Rev-erbɑ in lipid and glucose homeostasis, obesity, and metabolic
disorders syndrome. In conclusion, this paper aims to understand better the role and mechanism of Rev-erbɑ in regulating
drug metabolism, lipid, glucose homeostasis, obesity, and metabolic disorders syndrome, which explores how to target Rev-erbɑ
to guide the design and development of new drugs and provide scientific reference for the molecular mechanism of new
drug development, rational drug use, and drug interaction.
