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1.
A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors.
Armstrong, J I; Ge, X; Verdugo, D E; Winans, K A; Leary, J A; Bertozzi, C R.
Org Lett ; 3(17): 2657-60, 2001 Aug 23.
Article in English | MEDLINE | ID: mdl-11506602

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.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Sulfotransferases/antagonists & inhibitors , Aldehydes/chemistry , Enzyme Inhibitors/chemistry , Phosphoadenosine Phosphosulfate/chemistry , Substrate Specificity
2.
Discovery of estrogen sulfotransferase inhibitors from a purine library screen.
Verdugo, D E; Cancilla, M T; Ge, X; Gray, N S; Chang, Y T; Schultz, P G; Negishi, M; Leary, J A; Bertozzi, C R.
J Med Chem ; 44(17): 2683-6, 2001 Aug 16.
Article in English | MEDLINE | ID: mdl-11495578

Subject(s)
Enzyme Inhibitors/chemical synthesis , Purines/chemical synthesis , Sulfotransferases/antagonists & inhibitors , Chromatography, Thin Layer , Combinatorial Chemistry Techniques , Enzyme Inhibitors/chemistry , Enzymes, Immobilized , Mass Spectrometry , Purines/chemistry , Sepharose
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