A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors

Authors
Armstrong, JI Ge, X Verdugo, DE Winans, KA Leary, JA Bertozzi, CR
Citation
Ji. Armstrong et al., A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors, ORG LETT, 3(17), 2001, pp. 2657-2660
Citations number
23
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
ORGANIC LETTERS
ISSN journal
15237060 → ACNP
Volume
3
Issue
17
Year of publication
2001
Pages
2657 - 2660
Database
ISI
SICI code
1523-7060(20010823)3:17<2657:ALATTG>2.0.ZU;2-1
Abstract
[GRAPHICS] A library of potential bisubstrate analogue inhibitors (1) targeting sulfot ransferase enzymes was generated by the chemoselective ligation of the PAPS mimic 2 with a panel of 447 aldehydes. Preliminary screening has identifie d compounds that inhibit estrogen sulfotransferase (EST), an enzyme relevan t to breast cancer.