Differential Roles of Human Monoamine (M)-Form and Simple Phenol (P)-Form Phenol Sulfotransferases in Drug Metabolism

DOI PDF Web Site PubMed 4 Citations 28 References

Search this article

Abstract

Cytosolic sulfotransferases (STs) are traditionally known as Phase II drug-metabolizing or detoxifying enzymes that facilitate the removal of drugs and other xenobiotic compounds. In this study, we carried out a systematic investigation on the sulfation of drug compounds by two major human phenol STs (PSTs), the monoamine (M)-form and simple phenol (P)-form PSTs. Activity data obtained showed the differential substrate specificity of the two enzymes for the thirteen drug compounds tested. Kinetic studies revealed that the M-form PST displayed stereoselectivity for the chiral drug, isoproterenol. The effects of divalent metal cations on the activity of the M-form and P-form PSTs toward representative drug compounds were quantitatively evaluated. Results obtained indicated that the drug-sulfating activities of the two human PSTs were partially or completely inhibited or stimulated by the ten divalent metal cations tested at a 5 mM concentration. The two enzymes appeared to be less sensitive to the effects of physiologically more abundant metal cations such as Mg2+ and Ca2+, but more sensitive to the detrimental effects of other metal cations that may enter the body as environmental contaminants.

Journal

Citations (4)*help

See more

References(28)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top