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Published on: March 10, 2021
Replacing the pyrophosphate group of HMB-PP by a diphosphonate function abrogates Its potential to activate human
Armin Reichenberg1, Martin Hintz, Yvonne Kletschek
1Jomaa Pharmaka GmbH, Frankfurter Str. 50, D-35392 Giessen, Germany.
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.
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