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Quantitative characterization of UDP-glucuronosyltransferase 2B17 in human liver and intestine and its role in testosterone first-pass metabolism.


ABSTRACT: Protein abundance and activity of UGT2B17, a highly variable drug- and androgen-metabolizing enzyme, were quantified in microsomes, S9 fractions, and primary cells isolated from human liver and intestine by validated LC-MS/MS methods. UGT2B17 protein abundance showed >160-fold variation (mean?±?SD, 1.7?±?2.7?pmol/mg microsomal protein) in adult human liver microsomes (n?=?26) and significant correlation (r2?=?0.77, p?

SUBMITTER: Zhang H 

PROVIDER: S-EPMC6188809 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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Quantitative characterization of UDP-glucuronosyltransferase 2B17 in human liver and intestine and its role in testosterone first-pass metabolism.

Zhang Haeyoung H   Basit Abdul A   Busch Diana D   Yabut King K   Bhatt Deepak Kumar DK   Drozdzik Marek M   Ostrowski Marek M   Li Albert A   Collins Carol C   Oswald Stefan S   Prasad Bhagwat B  

Biochemical pharmacology 20180804


Protein abundance and activity of UGT2B17, a highly variable drug- and androgen-metabolizing enzyme, were quantified in microsomes, S9 fractions, and primary cells isolated from human liver and intestine by validated LC-MS/MS methods. UGT2B17 protein abundance showed >160-fold variation (mean ± SD, 1.7 ± 2.7 pmol/mg microsomal protein) in adult human liver microsomes (n = 26) and significant correlation (r<sup>2</sup> = 0.77, p < 0.001) with testosterone glucuronide (TG) formation. Primary role  ...[more]

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