Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism

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 μ...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (3), p.571-573
Main Authors: Norris, Andrew J., Whitelegge, Julian P., Strouse, M.Jane, Faull, Kym F., Toyokuni, Tatsushi
Format: Article
Language:English
Subjects:
Analytical, structural and metabolic biochemistry
Binding Sites
Binding, Competitive
Biological and medical sciences
Enzyme Inhibitors - pharmacology
Enzymes and enzyme inhibitors
Fucosyltransferases - antagonists & inhibitors
Fucosyltransferases - metabolism
Fundamental and applied biological sciences. Psychology
Guanosine Diphosphate Fucose - analogs & derivatives
Guanosine Diphosphate Fucose - pharmacology
Indicators and Reagents
Kinetics
Medical sciences
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Spectrometry, Mass, Electrospray Ionization
Substrate Specificity
Transferases
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Summary: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 μM, similar to the K m value for GDP-Fuc (50.4±5.5 μM), while the C-Fuc analogue exhibited significantly weak competitive inhibition with a K i value of 889±93 μM. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.12.003