SULT dimers sulfate APAP to APAP-SO3

Stable Identifier
Reaction [transition]
Homo sapiens
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After a therapeutic dose, a large fraction (30-44%) of acetaminophen (APAP) can be converted to inactive sulfate conjugates. Cytosolic sulfotransferases (SULTs) carry out the sulfation conjugation of APAP. SULTs transfer a sulfo group from PAPS to APAP, making it more polar and therefore easier to eliminate. SULTs 1A1, 1A3, 1A4, 1C4, 1E1 and 2A1 are known to have sulfotransferase activity towards APAP (Reiter & Weinshilboum 1992, Adjei et al. 2008, Mazaleuskaya et al. 2015). SULTs are expressed in many tissues but Yamamoto et al. found higher sulfating activity in the liver and intestine than that found in the lung and kidney (Yamamoto et al. 2015).
Literature References
PubMed ID Title Journal Year
26067475 Sulphation of acetaminophen by the human cytosolic sulfotransferases: a systematic analysis

Liu, MC, Liu, MY, Yamamoto, A, Kurogi, K, Saeki, Y, Suiko, M, Sakakibara, Y

J Biochem 2015
26049587 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses

Mazaleuskaya, LL, Klein, TE, Sangkuhl, K, FitzGerald, GA, Altman, RB, Thorn, CF

Pharmacogenet Genomics 2015
18232020 Interindividual variability in acetaminophen sulfation by human fetal liver: implications for pharmacogenetic investigations of drug-induced birth defects

Leeder, JS, Weinshilboum, RM, Simon, SD, Gaedigk, A, Adjei, AA

Birth Defects Res A Clin Mol Teratol 2008
6950087 Acetaminophen and phenol: substrates for both a thermostable and a thermolabile form of human platelet phenol sulfotransferase

Reiter, C, Weinshilboum, RM

J Pharmacol Exp Ther 1982
Catalyst Activity

sulfotransferase activity of SULT dimers (APAP) [cytosol]

Orthologous Events
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