Replacing the pyrophosphate group of HMB-PP by a diphosphonate function abrogates its potential to activate human γδ T cells but does not lead to competitive …

A Reichenberg, M Hintz, Y Kletschek, T Kuhl…

Index: Reichenberg, Armin; Hintz, Martin; Kletschek, Yvonne; Kuhl, Tanja; Haug, Christian; Engel, Rosel; Moll, Jens; Ostrovsky, Dmitry N.; Jomaa, Hassan; Eberl, Matthias Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 7 p. 1257 - 1260

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Citation Number: 44

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 EC50 of 0.1–0.2 nM, HMB-PP is significantly more potent in stimulating human Vγ9/Vδ2 T cells than any other compound described so far. However, replacing the pyrophosphate by a P–CH2–P function abrogates the bioactivity drastically, with HMB-PCP having a EC50 of ...