A library approach to the generation of bisubstrate analogue sulfotransferase inhibitors.
[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.
Armstrong
J I
JI
Department of Chemistry, University of California, Berkeley, California 94720, USA.
Ge
X
X
Verdugo
D E
DE
Winans
K A
KA
Leary
J A
JA
Bertozzi
C R
CR
D000447:Aldehydes / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D010724:Phosphoadenosine Phosphosulfate / Q000737:chemistry; D013379:Substrate Specificity; D015238:Sulfotransferases / Q000037:antagonists & inhibitors*
D000447:Aldehydes; D004791:Enzyme Inhibitors; D010724:Phosphoadenosine Phosphosulfate; D015238:Sulfotransferases; C020122:estrone sulfotransferase