Bioluminescent probes of sulfatase activity.

Sulfation of glycans, proteins, and small molecules is a biological regulatory modification that plays important roles in normal and disease processes.[1] The enzymes that install and hydrolyze sulfate esters are the sulfotransferases and sulfatases, respectively. The sulfatases in particular have been associated with a number of congenital and acquired disease states.[2] Steroid sulfatase inhibitors are under evaluation as anticancer drugs,[3] and the association of heparan sulfatases with cancer[2b, 4] suggests future opportunities for therapeutic approaches that target this enzyme class. Moreover, sulfatases are predicted from the genome sequences of many pathogenic microbes, including Mycobacterium tuberculosis,[5] although their biological functions are not well defined.