Fucosyltransferase-specific inhibition via next generation of fucose mimetics. Issue 9 (7th January 2021)

• Record Type: Journal Article
• Authors: Martin, Kyle C.; Tricomi, Jacopo; Corzana, Francisco; García-García, Ana; Ceballos-Laita, Laura; Hicks, Thomas; Monaco, Serena; Angulo, Jesus; Hurtado-Guerrero, Ramon; Richichi, Barbara; Sackstein, Robert
• Is Part Of: Chemical communications. Volume 57:Issue 9(2021)
• Page Start: 1145
• Page End: 1148
• Publication Date: 2021-01-07
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc04847j
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : A conformationally constrained mimetic of l -fucose has been employed to explore whether glycan mimicry could be utilized to interfere with the catalytic activity of α-1, 3-fucosyltransferases. Abstract : The ability to custom-modify cell surface glycans holds great promise for treatment of a variety of diseases. We propose a glycomimetic of l -fucose that markedly inhibits the creation of sLe X by FTVI and FTVII, but has no effect on creation of Le X by FTIX. Our findings thus indicate that selective suppression of sLex display can be achieved, and STD-NMR studies surprisingly reveal that the mimetic does not compete with GDP-fucose at the enzymatic binding site.