%0 Journal Article
%T Development of ¦Á-GalCer Analogues with an ¦Á-Fluorocarbonyl Moiety as Th2-Selective Ligands of CD1d
%J -
%D 2019
%R https://doi.org/10.1021/acsmedchemlett.9b00026
%X A series of ¦Á-GalCer analogues containing an ¦Á-fluorocarbonyl moiety at the terminal position of the acyl chain were designed for targeting polar residues in the hydrophobic cavity of CD1d using a structure-based approach. The acyl chain length was efficiently adjusted by an asymmetric alkyne¨Calkyne cross coupling strategy, and the newly synthesized ¦Á-GalCer analogues showed the high Th2-selective activity of iNKT cells. The biased activity of ligands could be caused by the hydrogen-bonding interaction between ligands and CD1d according to the Th2-selective cytokine secretion and molecular docking studies
%U https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00026