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  • Title: Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism.
    Author: Norris AJ, Whitelegge JP, Strouse MJ, Faull KF, Toyokuni T.
    Journal: Bioorg Med Chem Lett; 2004 Feb 09; 14(3):571-3. PubMed ID: 14741245.
    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.
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