中国科学院大连化学物理研究所机构知识库
Advanced  
DICP OpenIR  > 中国科学院大连化学物理研究所  > 期刊论文
题名: UGT1A10 Is a High Activity and Important Extrahepatic Enzyme: Why Has Its Role in Intestinal Glucuronidation Been Frequently Underestimated?
作者: Troberg, Johanna1;  Jarvinen, Erkka1;  Ge, Guang-Bo2;  Yang, Ling2;  Finel, Moshe1
关键词: UDP-glucuronosyltransferase ;  recombinant UGT1A10 ;  intestine microsomes ;  intestinal glucuronidation ;  estradiol ;  estrone ;  morphine ;  SN-38 ;  AMC ;  NCHN ;  bavachinin
刊名: MOLECULAR PHARMACEUTICS
发表日期: 2017-09-01
DOI: 10.1021/acs.molpharmaceut.6b00852
卷: 14, 期:9, 页:2875-2883
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Medicine, Research & Experimental ;  Pharmacology & Pharmacy
研究领域[WOS]: Research & Experimental Medicine ;  Pharmacology & Pharmacy
英文摘要: The aim of this work was to highlight a considerable and broad problem in UGT1A10 activity assessment that has led to underestimation of its role in intestinal glucuronidation of drugs and other xenobiotics. The reason appears to be poor activity of the commercial UGT1A10 that is used by many laboratories, and here we have tested it by comparison with our recombinant His-tagged UGT1A10 (designated as UGT1A10-H), both expressed in insect cells. The glucuronidation rates of morphine, estradiol, estrone, SN-38, diclofenac, 4-methylumbelliferone, 7-amino-4-methylcoumarin, N-(3-carboxypropyl)-4-hydroxy-1,8-naphthalimide, and bavachinin were assayed. The results revealed that the activity of commercial UGT1A10 was low, very low, and in the cases of morphine, estrone, 7-methyl-4-aminocoumarin, and bavachinin it was below the detection limit. On the other hand, under the same conditions, UGT1A10-H exhibited high glucuronidation rates toward all these compounds. Moreover, using estradiol, morphine, and estrone, in the presence and absence of suitable inhibitors, nilotinib or atractylenolide I, it was demonstrated that UGT1A10-H, but not the commercial UGT1A10, provides a good tool to study the role of native UGT1A10 in the human intestine. The results also suggest that much of the data in the literature on UGT1A10 activity may have to be re-evaluated.
关键词[WOS]: HUMAN UDP-GLUCURONOSYLTRANSFERASES ;  TANDEM MASS-SPECTROMETRY ;  TRANSFERASE 1A ;  HUMAN TISSUES ;  UGT ENZYMES ;  IN-VITRO ;  EXPRESSION ;  ISOFORMS ;  QUANTIFICATION ;  SELECTIVITY
语种: 英语
WOS记录号: WOS:000410005100003
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/150036
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.Univ Helsinki, Div Pharmaceut Chem & Technol, Fac Pharm, POB 56 Viikinkaari 5, Helsinki 00014, Finland
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

Recommended Citation:
Troberg, Johanna,Jarvinen, Erkka,Ge, Guang-Bo,et al. UGT1A10 Is a High Activity and Important Extrahepatic Enzyme: Why Has Its Role in Intestinal Glucuronidation Been Frequently Underestimated?[J]. MOLECULAR PHARMACEUTICS,2017,14(9):2875-2883.
Service
 Recommend this item
 Sava as my favorate item
 Show this item's statistics
 Export Endnote File
Google Scholar
 Similar articles in Google Scholar
 [Troberg, Johanna]'s Articles
 [Jarvinen, Erkka]'s Articles
 [Ge, Guang-Bo]'s Articles
CSDL cross search
 Similar articles in CSDL Cross Search
 [Troberg, Johanna]‘s Articles
 [Jarvinen, Erkka]‘s Articles
 [Ge, Guang-Bo]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
  Add to CiteULike  Add to Connotea  Add to Del.icio.us  Add to Digg  Add to Reddit 
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Powered by CSpace