Recent progress and challenges in screening and characterization of UGT1A1 inhibitors
文献类型：期刊论文
| 作者 | Finel, Moshe4; Lv, Xia1,2; Xia, Yangliu3; Wu, Jingjing3; Ge, Guangbo1,3; Yang, Ling1 |
| 刊名 | ACTA PHARMACEUTICA SINICA B
 |
| 出版日期 | 2019-03-01 |
| 卷号 | 9期号:2页码:258-278 |
| 关键词 | UGT1A1 inhibitors Drug/herbdrug interactions Probe substrates High-throughput screening |
| ISSN号 | 2211-3835 |
| DOI | 10.1016/j.apsb.2018.09.005 |
| 通讯作者 | Ge, Guangbo(geguangbo@shutcm.edu.cn) |
| 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. |
| WOS关键词 | UDP-GLUCURONOSYLTRANSFERASE 1A1 ; HUMAN LIVER-MICROSOMES ; RATIOMETRIC FLUORESCENT-PROBE ; PRIMARY HUMAN HEPATOCYTES ; HUMAN CARBOXYLESTERASE 2 ; IN-VITRO INHIBITION ; BILIRUBIN GLUCURONIDATION ; GENETIC-POLYMORPHISM ; DRUG-INTERACTIONS ; ENZYME-ACTIVITIES |
| 资助项目 | NSF of China[81773687] ; NSF of China[81703606] ; NSF of China[81573501] ; NSF of China[81473181] ; National Key Research and Development Program of China[2017YFC1700200] ; National Key Research and Development Program of China[2017YFC1702000] ; Fundamental Research Funds for the Central Universities[wd01185] ; National S&T Major Projects of China[2017ZX09101004] ; Program of Shanghai Academic/Technology Research Leader[18XD1403600] ; Innovative Entrepreneurship Program of High-level Talents in Dalian[2016RQ025] ; Innovative Entrepreneurship Program of High-level Talents in Dalian[2017RQ121] ; Doctoral Scientific Research Foundation of Liaoning Province, China[20170520059] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000461052500004 |
| 出版者 | INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES |
| 资助机构 | NSF of China ; NSF of China ; National Key Research and Development Program of China ; National Key Research and Development Program of China ; Fundamental Research Funds for the Central Universities ; Fundamental Research Funds for the Central Universities ; National S&T Major Projects of China ; National S&T Major Projects of China ; Program of Shanghai Academic/Technology Research Leader ; Program of Shanghai Academic/Technology Research Leader ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Doctoral Scientific Research Foundation of Liaoning Province, China ; Doctoral Scientific Research Foundation of Liaoning Province, China ; NSF of China ; NSF of China ; National Key Research and Development Program of China ; National Key Research and Development Program of China ; Fundamental Research Funds for the Central Universities ; Fundamental Research Funds for the Central Universities ; National S&T Major Projects of China ; National S&T Major Projects of China ; Program of Shanghai Academic/Technology Research Leader ; Program of Shanghai Academic/Technology Research Leader ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Doctoral Scientific Research Foundation of Liaoning Province, China ; Doctoral Scientific Research Foundation of Liaoning Province, China ; NSF of China ; NSF of China ; National Key Research and Development Program of China ; National Key Research and Development Program of China ; Fundamental Research Funds for the Central Universities ; Fundamental Research Funds for the Central Universities ; National S&T Major Projects of China ; National S&T Major Projects of China ; Program of Shanghai Academic/Technology Research Leader ; Program of Shanghai Academic/Technology Research Leader ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Doctoral Scientific Research Foundation of Liaoning Province, China ; Doctoral Scientific Research Foundation of Liaoning Province, China ; NSF of China ; NSF of China ; National Key Research and Development Program of China ; National Key Research and Development Program of China ; Fundamental Research Funds for the Central Universities ; Fundamental Research Funds for the Central Universities ; National S&T Major Projects of China ; National S&T Major Projects of China ; Program of Shanghai Academic/Technology Research Leader ; Program of Shanghai Academic/Technology Research Leader ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Innovative Entrepreneurship Program of High-level Talents in Dalian ; Doctoral Scientific Research Foundation of Liaoning Province, China ; Doctoral Scientific Research Foundation of Liaoning Province, China |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/165892]  |
| 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 |
| 通讯作者 | Ge, Guangbo |
| 作者单位 | 1.Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Med, Shanghai 201203, Peoples R China 2.Dalian Minzu Univ, Coll Life Sci, Minist Educ, Key Lab Biotechnol & Bioresources Utilizat, Dalian 116600, Peoples R China 3.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China 4.Univ Helsinki, Div Pharmaceut Chem & Technol, Fac Pharm, Helsinki, Finland |
| 推荐引用方式 GB/T 7714 | Finel, Moshe,Lv, Xia,Xia, Yangliu,et al. Recent progress and challenges in screening and characterization of UGT1A1 inhibitors[J]. ACTA PHARMACEUTICA SINICA B,2019,9(2):258-278. |
| APA | Finel, Moshe,Lv, Xia,Xia, Yangliu,Wu, Jingjing,Ge, Guangbo,&Yang, Ling.(2019).Recent progress and challenges in screening and characterization of UGT1A1 inhibitors.ACTA PHARMACEUTICA SINICA B,9(2),258-278. |
| MLA | Finel, Moshe,et al."Recent progress and challenges in screening and characterization of UGT1A1 inhibitors".ACTA PHARMACEUTICA SINICA B 9.2(2019):258-278. |
入库方式： OAI收割
来源：大连化学物理研究所
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