Recent progress in the discovery of natural inhibitors against human carboxylesterases
文献类型：期刊论文
| 作者 | Hou, Jie3; Yang, Ling1; Wang, Dan-Dan1,2; Zou, Li-Wei1,2; Jin, Qiang2; Ge, Guang-Bo2 |
| 刊名 | FITOTERAPIA
 |
| 出版日期 | 2017-03-01 |
| 卷号 | 117页码:84-95 |
| 关键词 | Carboxylesterases Hce1 Hce2 Natural Inhibitors High-throughput Screening |
| ISSN号 | 0367-326X |
| DOI | 10.1016/j.fitote.2017.01.010 |
| 文献子类 | Review |
| 英文摘要 | Mammalian carboxylesterases (CEs) are important serine hydrolases catalyzing the hydrolysis of ester- or amide-containing compounds into the corresponding alcohols and carboxylic acids. in human, two primary carboxylesterases including hCE1 and hCE2 have been identified and extensively studied in the past decade. hCE1 is known to play crucial roles in the metabolism of a wide variety of endogenous esters, clinical drugs and insecticides, while hCE2 plays a key role in the metabolic activation of anticancer agents including irinotecan and capecitabine. The key roles of hCEs in both human health and xenobiotic metabolism arouse great interest in the discovery of potent and selective hCEs inhibitors to modulate endobiotic metabolism or to improve the outcomes of patients administrated with ester drugs. This review covers the significance and recent progress in the discovery of natural inhibitors against hCEs. The tools for screening and characterization of inhibitors against human CEs, induding traditional LC-based approaches and the newly developed optical substrate-based assays, are summarized and discussed for the first time. Furthermore, the structural information and inhibitory capacities of all reported hCEs inhibitors including fatty acids, flavonoids, tanshinones and triterpenoids have been systematically summarized. All information and knowledge presented in this review will be very helpful for medicinal chemists to develop more potent and highly selective inhibitors against hCEs for potential biomedical applications. (C) 2017 Published by Elsevier B.V. |
| WOS关键词 | RATIOMETRIC FLUORESCENT-PROBE ; COMPLEX BIOLOGICAL SAMPLES ; MAMMALIAN CARBOXYLESTERASES ; HUMAN LIVER ; SELECTIVE-INHIBITION ; DRUG DISCOVERY ; BENZIL DIPHENYLETHANE-1,2-DIONE ; UDP-GLUCURONOSYLTRANSFERASE ; INTESTINAL CARBOXYLESTERASE ; ARYLACETAMIDE DEACETYLASE |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000395852600015 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/169444]  |
| 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 | Hou, Jie; Ge, Guang-Bo |
| 作者单位 | 1.Shanghai Univ Tradit Chinese Med, Shanghai 201210, Peoples R China 2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China 3.Dalian Med Univ, Dalian 116044, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hou, Jie,Yang, Ling,Wang, Dan-Dan,et al. Recent progress in the discovery of natural inhibitors against human carboxylesterases[J]. FITOTERAPIA,2017,117:84-95. |
| APA | Hou, Jie,Yang, Ling,Wang, Dan-Dan,Zou, Li-Wei,Jin, Qiang,&Ge, Guang-Bo.(2017).Recent progress in the discovery of natural inhibitors against human carboxylesterases.FITOTERAPIA,117,84-95. |
| MLA | Hou, Jie,et al."Recent progress in the discovery of natural inhibitors against human carboxylesterases".FITOTERAPIA 117(2017):84-95. |
入库方式： OAI收割
来源：大连化学物理研究所
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