Potential role of CYP1B1 in the development and treatment of metabolic diseases.
Cytochrome P450 1B1 (CYP1B1), a member of CYP superfamily, is expressed in liver and extrahepatic tissues carries out the metabolism of numerous xenobiotics, including metabolic activation of polycyclic aromatic hydrocarbons. Surprisingly, CYP1B1 was also shown to be important in regulating endogenous metabolic pathways, including the metabolism of steroid hormones, fatty acids, melatonin, and vitamins. CYP1B1 and nuclear receptors including peroxisome proliferator-activated receptors (PPARs), estrogen receptor (ER), and retinoic acid receptors (RAR) contribute to the maintenance of the homeostasis of these endogenous compounds. Many natural flavonoids and synthetic stilbenes show inhibitory activity toward CYP1B1 expression and function, notably isorhamnetin and 2,4,3',5'-tetramethoxystilbene. Accumulating evidence indicates that modulation of CYP1B1 can decrease adipogenesis and tumorigenesis, and prevent obesity, hypertension, atherosclerosis, and cancer. Therefore, it may be feasible to consider CYP1B1 as a therapeutic target for the treatment of metabolic diseases.
Laboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, China.
Fei
F
Li
Research Center for Differentiation and Development of Basic Theory of Traditional Chinese Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Weifeng
W
Zhu
Laboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA. Electronic address: gonzalef@mail.nih.gov.
Frank J
FJ
Gonzalez
D000818:Animals; D065633:Cytochrome P-450 CYP1B1 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006801:Humans; D008659:Metabolic Diseases / Q000188:drug therapy* / Q000378:metabolism; D008822:Mice, Transgenic
D065633:Cytochrome P-450 CYP1B1
CYP1B1; Metabolic diseases; Metabolic pathways; Metabolomics