A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors.

Academic Article

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

  • Armstrong, JI
  • Ge, X
  • Verdugo, DE
  • Winans, Katharine
  • Leary, JA
  • Bertozzi, CR

    • Status

    Publication Date

  • August 23, 2001

    • Has Subject Area

    Published In

  • Organic Letters  Journal

    • Keywords

  • Aldehydes
  • Enzyme Inhibitors
  • Phosphoadenosine Phosphosulfate
  • Substrate Specificity
  • Sulfotransferases

    • Digital Object Identifier (doi)

    Pubmed Id

  • 11506602

    • Start Page

  • 2657

    • End Page

  • 2660

    • Volume

  • 3

    • Issue

  • 17