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  • Title: Synthesis of a bisubstrate analogue targeting estrogen sulfotransferase.
    Author: Armstrong JI, Verdugo DE, Bertozzi CR.
    Journal: J Org Chem; 2003 Jan 10; 68(1):170-3. PubMed ID: 12515476.
    Abstract:
    Sulfotransferases catalyze the transfer of a sulfuryl group from the eukaryotic sulfate donor 3'-phosphoadenosine 5'-phosphosulfate to an acceptor biomolecule. Sulfotransferases have been linked with several disease states, prompting our investigation of specific sulfotransferase inhibitors. Presented herein is the synthesis and evaluation of a bisubstrate analogue designed to inhibit estrogen sulfotransferase. The synthesis utilizes a novel, orthogonally protected 3'-phosphoadenosine 5'-phosphate (PAP) derivative allowing the selective functionalization of the 5'-phosphate with a sulfate acceptor mimic. Kinetic studies revealed significant inhibitory activity and provide guidance for improved inhibitor design.
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