Identifying and applying a highly selective probe to simultaneously determine the O-glucuronidation activity of human UGT1A3 and UGT1A4

نویسندگان

  • Li Jiang
  • Si-Cheng Liang
  • Chao Wang
  • Guang-Bo Ge
  • Xiao-Kui Huo
  • Xiao-Yi Qi
  • Sa Deng
  • Ke-Xin Liu
  • Xiao-Chi Ma
چکیده

Glucuronidation mediated by uridine 5'-diphospho (UDP)-glucuronosyltransferase is an important detoxification pathway. However, identifying a selective probe of UDP- glucuronosyltransferase is complicated because of the significant overlapping substrate specificity displayed by the enzyme. In this paper, desacetylcinobufagin (DACB) 3-O- and 16-O-glucuronidation were found to be isoform-specific probe reactions for UGT1A4 and UGT1A3, respectively. DACB was well characterized as a probe for simultaneously determining the catalytic activities of O-glucuronidation mediated by UGT1A3 and UGT1A4 from various enzyme sources, through a sensitive analysis method.

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عنوان ژورنال:

دوره 5  شماره 

صفحات  -

تاریخ انتشار 2015