478050-96-3Relevant articles and documents
Synthesis of a bisubstrate analogue targeting estrogen sulfotransferase
Armstrong, Joshua I.,Verdugo, Dawn E.,Bertozzi, Carolyn R.
, p. 170 - 173 (2003)
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.
