Sulfation is an important conjugation reaction in the metabolism of various xenobiotics and endogenous compounds and is catalyzed by sulfotransferase (ST) present in cytosols. The cloning studies on STs have provided the basis for the understanding of the ST multigene family. STs are classified into hydroxysteroid (or alcohol), aryl (or phenol), estrogen, flavonol and polysaccharide STs and recent developments in the molecular characterization of these isoforms are reviewed. Regulation and localization of ST isoforms in various tissues are characterized at the molecular level by virtue of the specific antibodies and the corresponding cDNA probes. The recent developments are summarized. ST inhibitors are potent tools for the study on ST multiplicity and for the characterization of the enzyme structure. It also appears to be important to understand exogenous and endogenous ST inhibitors in clinical environment. The recent developments are reviewed.