2010
DOI: 10.1124/dmd.110.033829
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Abstract: ABSTRACT:Bilirubin, an end product of heme catabolism, is primarily eliminated via glucuronic acid conjugation by UGT1A1. Impaired bilirubin conjugation, caused by inhibition of UGT1A1, can result in clinical consequences, including jaundice and kernicterus. Thus, evaluation of the ability of new drug candidates to inhibit UGT1A1-catalyzed bilirubin glucuronidation in vitro has become common practice. However, the instability of bilirubin and its glucuronides presents substantial technical challenges to conduc… Show more

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Cited by 30 publications
(26 citation statements)
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“…Methods for quantitation of bilirubin monoglucuronides and diglucuronide were as described previously (Zhou et al, 2010a). Estradiol-3-glucuronide was quantified either through an LC-MS method with an LC-10ADVP system (Shimadzu, Columbia, MD) or through a capillary LC-MS/MS method (for estradiol and bilirubin interaction experiments only) on a TSQ Quantum Discovery Max MS system (Thermo Fisher Scientific) coupled with an Agilent 1100 capillary HPLC system (Agilent Technologies, Santa Clara, CA).…”
Section: Methodsmentioning
confidence: 99%
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“…Methods for quantitation of bilirubin monoglucuronides and diglucuronide were as described previously (Zhou et al, 2010a). Estradiol-3-glucuronide was quantified either through an LC-MS method with an LC-10ADVP system (Shimadzu, Columbia, MD) or through a capillary LC-MS/MS method (for estradiol and bilirubin interaction experiments only) on a TSQ Quantum Discovery Max MS system (Thermo Fisher Scientific) coupled with an Agilent 1100 capillary HPLC system (Agilent Technologies, Santa Clara, CA).…”
Section: Methodsmentioning
confidence: 99%
“…Supernatant from each sample (5 l) were injected onto the HPLC system for quantification. Detailed incubation conditions for bilirubin glucuronidation were as described previously (Zhou et al, 2010a). Bilirubin incubations were conducted with 0.05 mg/ml protein for 5 min.…”
Section: Methodsmentioning
confidence: 99%
“…Peaks were assigned based on the lipophilicity of the glucuronides and retention times reported previously. [12][13][14]16,20) Bilirubin and all metabolites were also identified using MS in the present study (Figs. 3, 4).…”
Section: Qualitation and Quantification Of Billirubin Monoglucuronidementioning
confidence: 99%
“…The parameters V max and K m were defined as the maximum velocity and the substrate concentration at which the velocity equaled half of the maximum velocity, respectively. 13,14,[18][19][20] The intrinsic clearance (CL int ) was calculated as V max /K m when the reaction exhibited Michaelis-Menten kinetics. …”
Section: µM)mentioning
confidence: 99%
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