Discovery of estrogen sulfotransferase inhibitors from a purine library screen.

نویسندگان

  • D E Verdugo
  • M T Cancilla
  • X Ge
  • N S Gray
  • Y T Chang
  • P G Schultz
  • M Negishi
  • J A Leary
  • C R Bertozzi
چکیده

Center for New Directions in Organic Synthesis, Howard Hughes Medical Institute, and Departments of Chemistry and Molecular and Cell Biology, University of California, Berkeley, California 94720, Genomics Institute of the Novartis Research Foundation, 3115 Merryfield Row, Suite 200, San Diego, California 92121, Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709, and Department of Chemistry, New York University, 100 Washington Square East, New York, New York 10003

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Discovery of Carbohydrate Sulfotransferase Inhibitors from a Kinase-Directed Library We thank Sharon Long and Dave Keating for providing both the NodH sulfotransferase and APS Kinase during our preliminary experiments and Jack Kirsch for numerous helpful conversations. J.I.A. and K.G.B were supported by NIH Molecular Biophysics Training Grant (No. T32GM0895). This research was funded by grants to C.R.B. from the Pew Scholars Program, the W. M. Keck Foundation and the American Cancer Society (Grant No. RPG9700501BE).

Carbohydrate sulfotransferases have recently emerged as an important and relatively unexplored class of therapeutic targets.[1] For example, the seminal discovery that sulfated sialyl LewisX mediates the adhesion of leukocytes to inflamed endothelium established carbohydrate sulfotransferases as potential targets for anti-inflammatory therapy.[2] Ongoing genome sequencing projects have uncovere...

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عنوان ژورنال:
  • Journal of medicinal chemistry

دوره 44 17  شماره 

صفحات  -

تاریخ انتشار 2001