recentprogressandchallengesinscreeningandcharacterizationofugt1a1inhibitors
文献类型：期刊论文
| 作者 | Lv Xia2; Xia Yangliu1; Finel Moshe3; Wu Jingjing1; Ge Guangbo2; Yang Ling2 |
| 刊名 | actapharmaceuticasinicab
 |
| 出版日期 | 2019-01-01 |
| 卷号 | 9期号:2页码:258 |
| ISSN号 | 2211-3835 |
| 英文摘要 | Uridine-diphosphate glucuronosyltransferase 1a1 (ugt1a1) is an important conjugative enzyme in mammals that is responsible for the conjugation and detoxification of both endogenous and xenobiotic compounds. strong inhibition of ugt1a1 may trigger adverse drug/herb-drug interactions, or result in metabolic disorders of endobiotic metabolism. therefore, both the us food and drug administration (fda) and the european medicines agency (ema) have recommended assaying the inhibitory potential of drugs under development on the human ugt1a1 prior to approval. this review focuses on the significance, progress and challenges in discovery and characterization of ugt1a1 inhibitors. recent advances in the development of ugt1a1 probes and their application for screening ugt1a1 inhibitors are summarized and discussed in this review for the first time. furthermore, a long list of ugt1a1 inhibitors, including information on their inhibition potency, inhibition mode, and affinity, has been prepared and analyzed. challenges and future directions in this field are highlighted in the final section. the information and knowledge that are presented in this review provide guidance for rational use of drugs/herbs in order to avoid the occurrence of adverse effects via ugt1a1 inhibition, as well as presenting methods for rapid screening and characterization of ugt1a1 inhibitors and for facilitating investigations on ugt1a1-ligand interactions. (c) 2019 chinese pharmaceutical association and institute of materia medica, chinese academy of medical sciences. production and hosting by elsevier b.v. |
| 语种 | 英语 |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/176394]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 作者单位 | 1.中国科学院大连化学物理研究所 2.上海中医药大学 3.赫尔辛基大学 |
| 推荐引用方式 GB/T 7714 | Lv Xia,Xia Yangliu,Finel Moshe,et al. recentprogressandchallengesinscreeningandcharacterizationofugt1a1inhibitors[J]. actapharmaceuticasinicab,2019,9(2):258. |
| APA | Lv Xia,Xia Yangliu,Finel Moshe,Wu Jingjing,Ge Guangbo,&Yang Ling.(2019).recentprogressandchallengesinscreeningandcharacterizationofugt1a1inhibitors.actapharmaceuticasinicab,9(2),258. |
| MLA | Lv Xia,et al."recentprogressandchallengesinscreeningandcharacterizationofugt1a1inhibitors".actapharmaceuticasinicab 9.2(2019):258. |
入库方式： OAI收割
来源：大连化学物理研究所
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