Human phenol sulfotransferases: chiral substrates and expression in Hep G2 cells.

ABSTRACT

Enzymatic sulfation of chiral phenolic ethanolamine drugs, e.g. beta-agonists, has been shown to be stereoselective in humans. The reaction appears to be specific for the monoamine (M) form of the phenol sulfotransferases (PSTs). In further studies of the stereochemistry of this reaction, we have found the hepatoblastoma-derived cell line Hep G2 to be an excellent human model. These cells contain the M form PST in quantities exceeding those of human liver by about 4-fold. Thus, sulfate conjugates of the beta-agonist drugs can easily be synthesized for subsequent structural and enzyme kinetic studies. Although less abundant, the phenol (P) form PST as well as dehydroepiandrosterone sulfotransferase are also expressed in the Hep G2 cells.