2015
DOI: 10.1248/bpb.b15-00513
|View full text |Cite
|
Sign up to set email alerts
|

Abstract: Estimating the extent to which drugs inhibit uridine 5′-diphosphate-glucuronosyltransferases1A1 (UGT1A1) enzyme activity is important for predicting hepatotoxicity and neurotoxicity. UGT1A1 enzyme activity is commonly evaluated by detecting the elimination of bilirubin substrate or the generation of bilirubin glucuronides. However, the present methods are inadequate for accurately assessing bilirubin metabolism, selecting incubation conditions, and comparing different systems. Therefore, in our study, we first… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1
1

Citation Types

3
7
0

Year Published

2017
2017
2022
2022

Publication Types

Select...
5
1

Relationship

1
5

Authors

Journals

citations
Cited by 12 publications
(10 citation statements)
references
References 19 publications
3
7
0
Order By: Relevance
“…We previously established a complete ultra-performance liquid chromatography (UPLC) method to detect bilirubin glucuronides for the purpose of analyzing the kinetic parameters of UGT1A1 41 . Chromatographic analyses were carried out using an Acquity UPLC system (Waters, Milford, MA, USA) equipped with a binary pump, automatic sampler, photo-diode array detector, system controller, and temperature-controlled oven.…”
Section: Methodsmentioning
confidence: 99%
See 3 more Smart Citations
“…We previously established a complete ultra-performance liquid chromatography (UPLC) method to detect bilirubin glucuronides for the purpose of analyzing the kinetic parameters of UGT1A1 41 . Chromatographic analyses were carried out using an Acquity UPLC system (Waters, Milford, MA, USA) equipped with a binary pump, automatic sampler, photo-diode array detector, system controller, and temperature-controlled oven.…”
Section: Methodsmentioning
confidence: 99%
“…UGT1A1 activity assays were conducted at 37 °C in a shaking water bath 41 . Incubation mixtures (final volume, 0.2 mL) contained 0.5 mg/mL RLM, 0.1 M Tris-HCl (pH 7.4), 5 mM MgCl 2 , 5 mM d -saccharic acid 1,4-lactone, 3.5 mM UDPGA, and 50 mg/g protein alamethicin.…”
Section: Methodsmentioning
confidence: 99%
See 2 more Smart Citations
“… Probe substrate Enzyme source Kinetic parameter Kinetic behavior Ref. K m or S 50 (μmol/L) V max (pmol/min/mg) 4-MU UGT1A1 113 308 Michaelis-Menten 48 Bilirubin UGT1A1 0.1 70 Michaelis-Menten 49 HLM 0.3 210 Michaelis-Menten 49 17 β -Estradiol UGT1A1 13 1300 Hill 50 HLM 11 820 Hill 50 Ethinylestradiol UGT1A1 9.7 600 Hill 51 HLM 13 1200 Hill 51 Etoposide UGT1A1 285 124 Michaelis-Menten 30 HLM 530 110 Michaelis-Menten 30 3,3′,4′-Trihydroxyflavone UGT1A1 1.53 1920 Substrate Inhibition 53 HLM 1.75 1990 Substrate Inhibition 53 3,6,4′-Trihydroxyflavone UGT1A1 0.76 340 Substrate Inhibition 53 HLM 0.83 ...…”
Section: Recent Progress In the Development Of Ugt1a1 Probe Substratementioning
confidence: 99%