Journal
PHARMACOLOGY & THERAPEUTICS
Volume 178, Issue -, Pages 18-30Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.pharmthera.2017.03.007
Keywords
CYP1B1; Metabolic diseases; Metabolic pathways; Metabolomics
Categories
Funding
- National Cancer Institute Intramural Research Program
- National Natural Science Foundation of China [81360509]
- Thousand Young Talents Program of China
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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. Published by Elsevier Inc.
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