title: Tyrosylprotein sulfotransferase inhibitors generated by combinatorial target-guided ligand assembly.
abstract: Tyrosylprotein sulfotransferases (TPSTs) catalyze the sulfation of tyrosine residues within secreted and membrane-bound proteins. The modification modulates protein-protein interactions in the extracellular environment. Here we use combinatorial target-guided ligand assembly to discover the first known inhibitors of human TPST-2.
authors.affiliation: Department of Molecular and Cell Biology, University of California, Berkeley, CA 94720, USA.
authors.forename: John W
authors.initials: JW
authors.lastname: Kehoe
authors.forename: Dustin J
authors.initials: DJ
authors.lastname: Maly
authors.forename: Dawn E
authors.initials: DE
authors.lastname: Verdugo
authors.forename: Joshua I
authors.initials: JI
authors.lastname: Armstrong
authors.forename: Brian N
authors.initials: BN
authors.lastname: Cook
authors.forename: Ying-Bin
authors.initials: YB
authors.lastname: Ouyang
authors.forename: Kevin L
authors.initials: KL
authors.lastname: Moore
authors.forename: Jonathan A
authors.initials: JA
authors.lastname: Ellman
authors.forename: Carolyn R
authors.initials: CR
authors.lastname: Bertozzi
mesh_terms: D000447:Aldehydes / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007202:Indicators and Reagents; D008024:Ligands; D015238:Sulfotransferases / Q000037:antagonists & inhibitors*
chemical_list: D000447:Aldehydes; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D008024:Ligands; D015238:Sulfotransferases; C039079:protein-tyrosine sulfotransferase; C020122:estrone sulfotransferase