title: A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors.
abstract: [reaction: see text]. A library of potential bisubstrate analogue inhibitors (1) targeting sulfotransferase enzymes was generated by the chemoselective ligation of the PAPS mimic 2 with a panel of 447 aldehydes. Preliminary screening has identified compounds that inhibit estrogen sulfotransferase (EST), an enzyme relevant to breast cancer.
authors.affiliation: Department of Chemistry, University of California, Berkeley, California 94720, USA.
authors.forename: J I
authors.initials: JI
authors.lastname: Armstrong
authors.forename: X
authors.initials: X
authors.lastname: Ge
authors.forename: D E
authors.initials: DE
authors.lastname: Verdugo
authors.forename: K A
authors.initials: KA
authors.lastname: Winans
authors.forename: J A
authors.initials: JA
authors.lastname: Leary
authors.forename: C R
authors.initials: CR
authors.lastname: Bertozzi
mesh_terms: D000447:Aldehydes / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D010724:Phosphoadenosine Phosphosulfate / Q000737:chemistry; D013379:Substrate Specificity; D015238:Sulfotransferases / Q000037:antagonists & inhibitors*
chemical_list: D000447:Aldehydes; D004791:Enzyme Inhibitors; D010724:Phosphoadenosine Phosphosulfate; D015238:Sulfotransferases; C020122:estrone sulfotransferase