Replacing the pyrophosphate group of HMB-PP by a diphosphonate function abrogates Its potential to activate human gammadelta T cells but does not lead...
Basic Information
ID: ALA1136675
Journal: Bioorg Med Chem Lett
Title: Replacing the pyrophosphate group of HMB-PP by a diphosphonate function abrogates Its potential to activate human gammadelta T cells but does not lead to competitive antagonism.
Authors: Reichenberg A, Hintz M, Kletschek Y, Kuhl T, Haug C, Engel R, Moll J, Ostrovsky DN, Jomaa H, Eberl M.
Abstract: The immunological characterization of (E)-4-hydroxy-3-methyl-but-2-enyl pyrophosphate (HMB-PP), and its methylenediphosphonate analogue, HMB-PCP, is described. With an EC(50) of 0.1-0.2 nM, HMB-PP is significantly more potent in stimulating human Vgamma9/Vdelta2 T cells than any other compound described so far. However, replacing the pyrophosphate by a P-CH(2)-P function abrogates the bioactivity drastically, with HMB-PCP having a EC(50) of only 5.3 microM.
CiteXplore: 12657258
DOI: 10.1016/s0960-894x(03)00138-0
Patent ID: ┄