Sulfotransferase (SULT)

Sulfate conjugation of xenobiotics is a phase-II metabolic reaction wherein cytosolic sulfotransferase enzymes (SULTs) transfer a sulfate group, typically from 3'-phosphoadenosine-5'-phosphosulfate (PAPS), to a hydroxyl or amine group on a xenobiotic or endogenous compound. This process generally increases the compound's water solubility, aiding its excretion from the body, and is essential for drug detoxification and hormonal homeostasis. However, sulfation can also produce chemically-reactive intermediates capable of inducing toxicity or adverse reactions, making SULTs key enzymes both in drug safety and pharmacogenetics[2][3][4][6][7][8][1]. Eleven major human SULT isoforms exist, differing in tissue distribution, substrate specificity, genetic variation, with important roles in drug metabolism, risk of toxicity, and variable drug response across individuals[2][3].

Other names

SulfationSulfonationO-sulfonationPhase-II sulfate conjugation

For substrate drugs: sulfation reduces toxicity and enhances excretion. For prodrugs (or pro-carcinogens): sulfation can bioactivate to toxic intermediates.