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Ligand mycophenolic acid O-acyl-glucuronide Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Basic Ligand Information
C2 3 H2 8 O1 2
mycophenolic acid O-acyl-glucuronide
QBMSTEZXAMABFF-UEARNRKISA-N
mycophenolic acid-acyl-glucuronide, mycophenoloyl beta-D-glucuronoside
Roles as Enzyme Ligand
In Vivo Product in Enzyme-catalyzed Reactions (1 result)
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UDP-glucuronate + mycophenolic acid = UDP + mycophenolic acid-acyl-glucuronide
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Substrate in Enzyme-catalyzed Reactions (1 result)
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mycophenolic acid O-acyl-glucuronide + H2O = mycophenolic acid + D-glucuronate
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Product in Enzyme-catalyzed Reactions (2 results)
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UDP-glucuronate + mycophenolic acid = UDP + mycophenolic acid-acyl-glucuronide
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UDP-glucuronate + mycophenolic acid = UDP + mycophenoloyl beta-D-glucuronoside
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Inhibitor in Enzyme-catalyzed Reactions (2 results)
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cross-reactivity by mycophenolic acid is less than 5%, thus interference is expected to be clinically irrelevant
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uncompetitive inhibition, is a weaker inhibitor of IMPDH II than mycophenolic acid. When coincubated with mycophenolic acid, mycophenolic acid-acyl-glucuronide activity is negligible at pharmacological concentrations
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Enzyme Kinetic Parameters
KM Value (1 result)
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0.1007
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recombinant enzyme, in 100 mM Tris-HCl (pH 7.4), at 37°C
Ki Value (2 results)
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0.000382
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in the presence of NAD+
0.000511
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in the presence of inosine 5'-phosphate
References & Links Literature References (3)
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Effect of mycophenolate acyl-glucuronide on human recombinant type 2 inosine monophosphate dehydrogenase
2009
Gensburger, O.; Picard, N.; Marquet, P.
Clin. Chem.
55
986-993
Multicenter evaluation of a new inosine monophosphate dehydrogenase inhibition assay for quantification of total mycophenolic acid in plasma
2008
Brandhorst, G.; Marquet, P.; Shaw, L.M.; Liebisch, G.; Schmitz, G.; Coffing, M.J.; Domke, I.; Streit, F.; Luthe, H.; Oellerich, M.
Ther. Drug Monit.
30
428-433
Human alpha/beta hydrolase domain containing 10 (ABHD10) is responsible enzyme for deglucuronidation of mycophenolic acid acyl-glucuronide in liver
2012
Iwamura, A.; Fukami, T.; Higuchi, R.; Nakajima, M.; Yokoi, T.
J. Biol. Chem.
287
9240-9249
Links to other databases for mycophenolic acid O-acyl-glucuronide