Research progress of human cytochrome P450 2J2 and its ligands
10.16438/j.0513-4870.2016-0573
- VernacularTitle:人细胞色素P450酶2J2的功能及其配体研究进展
- Author:
Hong-ying MA
1
;
Jing NING
2
;
Guang-bo GE
2
;
Ling YANG
2
;
Da-cheng HAO
1
Author Information
1. School of Environment and Chemical Engineering, Dalian Jiaotong University, Dalian 116028, China
2. Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China
- Publication Type:SPECIAL REPORTS
- Keywords:
CYP2J2;
metabolism;
human disease;
probe substrate;
CYP2J2 inhibitor
- From:
Acta Pharmaceutica Sinica
2017;52(1):26-33
- CountryChina
- Language:Chinese
-
Abstract:
Cytochrome P4502J2 (CYP2J2) is widely distributed in various human tissues and takes a part in the metabolism of endogenous compounds and drugs. CYP2J2 can convert arachidonic acid (AA) to expoxyeicosatrienoic acids (EETs), which have various biological effects, implying the important role of CYP2J2 in the regulation of cardiovascular system and promotion of tumor progression and metastasis. Additionally, CYP2J2 plays an indispensable role in the intestinal metabolism of various drugs, such as astemizole, terfenadine and ebastine. In this review, the metabolic function, characteristic of catalysis and tissue distribution of CYP2J2 are discussed with the latest literatures both in China and abroad. The state-of-the-art methods for characterization of CYP2J2 and current trend of substrate discovery as well as its relationship with disease are highlighted. This review gives in-depth understanding of the function of CYP2J2 and its role in disease advance. The information of ligand (substrate and inhibitor) will provide the theoretical guidance and reference to the development of novel drugs for CYP2J2.
