Organic Letters · 2001 · 33 citations · 16 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryEnzymologyDrug-metabolizing EnzymesEnzyme DiscoveryEnzyme InhibitionEnzyme ScreeningEnzyme TargetsEnzyme-substrate RecognitionChemoselective CouplingEnzyme Inhibition ScreeningEnzyme Inhibitor SynthesisEnzymesEstrogen MetabolitesEstrogen PharmacologyInhibitor ScreeningSulfotransferase Activity
[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.
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Tyrosine Sulfation of the Amino Terminus of CCR5 Facilitates HIV-1 Entry
Michael Farzan, Tajib A. Mirzabekov, Peter Kolchinsky et al. · Cell · 1999 · 698 citations · Full text
Mechanism-based design of a protein kinase inhibitor.
Stevan R. Hubbard, Philip A. Cole, Keykavous Parang et al. · Nature Structural Biology · 2001 · 192 citations
Conserved structural motifs in the sulfotransferase family
Yoshimitsu Kakuta, Lee G. Pedersen, Lars C. Pedersen et al. · Trends in Biochemical Sciences · 1998 · 175 citations