UGTs glucuronate APAP to APAP-GlcA

Stable Identifier
Reaction [transition]
Homo sapiens
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The liver, and to a lesser extent the kidney and intestine, are the major organs implicated in the elimination of acetaminophen (APAP, aka paracetamol) (McGill & Jaeschke 2013). Glucuronidation is the main route of APAP elimination, accounting for 45-55% of APAP metabolism, and is mediated by UGT1A1, UGT1A6, UGT1A9, UGT2B15 in the liver and UGT1A10 in the gut (Mutlib et al. 2006, Court et al. 2001, Navarro et al. 2011). Glucuronidation renders APAP more water-soluble, facilitating its elimination from the body.
Literature References
PubMed ID Title Journal Year
11714888 Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms

Greenblatt, DJ, Patten, CJ, Duan, SX, von Moltke, LL, Court, MH, Miners, JO, Mackenzie, PI

J Pharmacol Exp Ther 2001
16696573 Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity

Kulkarni, S, Kostrubsky, S, Mutlib, AE, Williams, JA, Goosen, TC, Bauman, JN

Chem Res Toxicol 2006
21666065 UGT1A6 and UGT2B15 polymorphisms and acetaminophen conjugation in response to a randomized, controlled diet of select fruits and vegetables

Potter, JD, Lampe, JW, Navarro, SL, King, IB, Chen, Y, Li, SS, Bigler, J, Chang, JL, Li, L, Schwarz, Y

Drug Metab Dispos 2011
Catalyst Activity

glucuronosyltransferase activity of UGTs (APAP substrate) [endoplasmic reticulum membrane]

Orthologous Events
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