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

Authors :: Armstrong JI
Ge X
Verdugo DE
Winans KA
Leary JA
Bertozzi CR
Source :: Organic letters [Org Lett] 2001 Aug 23; Vol. 3 (17), pp. 2657-60.
Publication Year :: 2001
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.

Subjects :: Aldehydes chemistry
Enzyme Inhibitors chemistry
Phosphoadenosine Phosphosulfate chemistry
Substrate Specificity
Enzyme Inhibitors chemical synthesis
Sulfotransferases antagonists & inhibitors

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