Synthesis and Evaluation of Transition-State Analogue Inhibitors of α-1,3-Fucosyltransferase This work was supported by the NIH and the Skaggs Institute. M.L.M. acknowledges fellowships from UNCFâMerck Science Initiative and Skaggs Predoctoral Fellows Program.

Abstract

Mimics of the geometry or charge of the fucose moiety of GDP-fucose in the transition state of fucosyltransferase-catalyzed reactions, compounds 1–3 are good competive inhibitors of α-1,3-fucosyltransferases V and VI with Ki values between 6 and 13 μM. GDP=guanosine diphosphate. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2002/z19273_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.