Reactome | UGTs glucuronate APAP to APAP-GlcA

UGTs glucuronate APAP to APAP-GlcA

Stable Identifier

R-HSA-158546

Type

Reaction [transition]

Species

Homo sapiens

Compartment

cytosol, endoplasmic reticulum membrane

ReviewStatus

5/5

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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