A potent and highly selective sulfotransferase inhibitor

Academic Article

Ding, Sheng, Ph.D. in Chemistry, Scripps Research 1999 - 2003
Chapman, Eli, Ph.D. in Chemistry, Scripps Research , Transferred from Columbia University 1998 - 2002

In the present work, we have used a newly developed, fluorescence-based assay to screen a library of >30 000 compounds as potential beta-arylsulfotransferase-IV inhibitors. A total of 11 inhibitors were discovered. Most of the compounds discovered showed low micromolar inhibition, but one of the compounds showed potent inhibition (Ki = 96 nM). The most potent of these inhibitors was tested against a variety of other purine binding enzymes and showed remarkable specificity.

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