2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2003 Apr 7;13(7):1257-60. doi: 10.1016/s0960-894x(03)00138-0.
Armin Reichenberg 1,  Martin Hintz,  Yvonne Kletschek,  Tanja Kuhl,  Christian Haug,  Rosel Engel,  Jens Moll,  Dmitry N Ostrovsky,  Hassan Jomaa,  Matthias Eberl
Affiliations

Affiliation

  • 1 Jomaa Pharmaka GmbH, Frankfurter Str. 50, D-35392 Giessen, Germany.
PMID: 12657258 DOI: 10.1016/s0960-894x(03)00138-0
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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