title: Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism.
abstract: Inhibition kinetics of two isosteric analogues of GDP-fucose (GDP-Fuc) were investigated against fucosyltransferase V using electrospray ionization mass spectrometry coupled to multiple reaction monitoring. The carba-Fuc analogue was found to be a competitive inhibitor with a K(i) value of 67.1+/-9.8 microM, similar to the K(m) value for GDP-Fuc (50.4+/-5.5 microM), while the C-Fuc analogue exhibited significantly weak competitive inhibition with a K(i) value of 889+/-93 microM.
authors.affiliation: Department of Molecular and Medical Pharmacology, David Geffen School of Medicine at University of California, Los Angeles, CA 90095, USA.
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Norris
authors.forename: Julian P
authors.initials: JP
authors.lastname: Whitelegge
authors.forename: M Jane
authors.initials: MJ
authors.lastname: Strouse
authors.forename: Kym F
authors.initials: KF
authors.lastname: Faull
authors.forename: Tatsushi
authors.initials: T
authors.lastname: Toyokuni
mesh_terms: D001665:Binding Sites; D001667:Binding, Competitive; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005647:Fucosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006154:Guanosine Diphosphate Fucose / Q000031:analogs & derivatives / Q000494:pharmacology*; D007202:Indicators and Reagents; D007700:Kinetics; D015394:Molecular Structure; D021241:Spectrometry, Mass, Electrospray Ionization; D013379:Substrate Specificity
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D006154:Guanosine Diphosphate Fucose; D005647:Fucosyltransferases; C435083:fucosyltransferase V