N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification
文献类型：期刊论文
| 作者 | Danyi Lu; Baojian Wu; Qian Xie |
| 刊名 | Journal of Pharmaceutical and Biomedical Analysis
 |
| 出版日期 | 2017 |
| 文献子类 | 期刊论文 |
| 英文摘要 | N-glucuronidation is an important pathway for metabolism and disposition of tertiary amines in humans.This reaction is mainly catalyzed by the enzymes UGT1A4 and UGT2B10. However, the metabolic patternsof UGT1A4- and UGT2B10-mediated N-glucuronidation are not fully clear. In this study, we first optimizedin vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine forUGT1A4, cotinine and amitriptyline for UGT2B10). Furthermore, we found that hepatic N-glucuronidationshowed significant species differences. In addition, UGT1A4 and UGT2B10 were primarily responsible forN-glucuronidation of many tertiary amines, including asenapine, loxapine, clozapine, chlorpromazine,dothiepin, doxepin, mirtazapine, mianserin, chlorcyclizine, cyclizine, promethazine, cyclobenzaprine,imatinib, retrorsine, strychnine and brucine. In conclusion, this study provides an in vitro assay systemfor evaluating N-glucuronidation of amines. Also, UGT1A4- and UGT2B10-mediated N-glucuronidationmight play significant roles in metabolism and detoxification of tertiary amines in humans. |
| URL标识 | 查看原文 |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/12268]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 作者单位 | Journal of Pharmaceutical and Biomedical Analysis |
| 推荐引用方式 GB/T 7714 | Danyi Lu,Baojian Wu,Qian Xie. N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification[J]. Journal of Pharmaceutical and Biomedical Analysis,2017. |
| APA | Danyi Lu,Baojian Wu,&Qian Xie.(2017).N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification.Journal of Pharmaceutical and Biomedical Analysis. |
| MLA | Danyi Lu,et al."N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification".Journal of Pharmaceutical and Biomedical Analysis (2017). |
入库方式： OAI收割
来源：深圳先进技术研究院
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