Transcriptional Profile of CYP3As and Functional Ezpression of CYP3A29 from Piglets
Expression profile of CYP3A individuals from piglets and characterization of CYP3A29 were investigated. Real-Time PCR showed that the liver and small intestines present the highest expression levels of CYP3A29, a human CYP3A4 homolog. The CYP3A29 was functional expressed in Bac-to-Bac baculovirus expression system together with NADPH p450 reductase (NPR) and cytochrome b5. For nifedipine oxidation (NOD) activity, recombinant CYP3A29 system showed similar enzyme kinetic parameters (Km=14.1～25.3 μM) to human recombinant CYP3A4, and a little variant to liver microsomes (Km=29.6～45.2 μM) from piglets. The NOD activity of recombinant CYP3A29 was strongly inhibited by ketoconazole (KET) and troleandomycin (TAO), and was slightly changed by inhibitors for other p450 enzymes from human. These results provided in detailed information of the characterizations of CYP3A29. We conclude from these results that caution should be hold when specific inhibitors or probes for human p450 enzymes are employed to investigate the veterinary drug metabolism.
CYP3As CYP3A29 heterologous ezpression characterization
Min Yao Zonghui Yuan Zhaoying Liu Menghong Dai Lingli Huang Dongmei Chen Yulian Wang Yanfei Tao Xu Wang Zhenli Liu
National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory of Food Safety Evaluation,Huazhong Agricultural University,Wuhan 430070,China
国际会议
北京
英文
1-4
2009-06-11（万方平台首次上网日期，不代表论文的发表时间）