Synthesis and immunological evaluation of the 4-β-glucoside of HMBPP

Bioorg Med Chem Lett. 2012 Jan 15;22(2):811-3. doi: 10.1016/j.bmcl.2011.12.055. Epub 2011 Dec 17.

Abstract

HMBPP ((E)-4-hydroxy-3-methyl-2-butenyl pyrophosphate) is a highly potent innate immunogen that stimulates human γδ T cells expressing the Vγ2Vδ2 T cell antigen receptor. To determine if glycoside conjugates of HMBPP retain activity, the 4-β-glucoside and its acetylated homolog were synthesized and tested for their ability to stimulate γδ T cells. The glycoside HMBPP conjugate stimulated human γδ T cells with an EC(50) of 78nM. The tetraacetyl glycoside HMBPP conjugate was also active (EC(50)=360nM). The two isomeric mono-β-glucosides of the parent (E)-2-methylbut-2-ene-1,4-diol, however, were not active. Thus, HMBPP glycosylated at the 4-OH position stimulates γδ T cells as long as the pyrophosphate moiety is present.

Publication types

  • Evaluation Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cell Line
  • Humans
  • Organophosphates / chemical synthesis*
  • Organophosphates / chemistry
  • Organophosphates / immunology*
  • Organophosphates / pharmacology
  • T-Lymphocytes / drug effects
  • T-Lymphocytes / immunology

Substances

  • 4-hydroxy-3-methyl-2-butenyl diphosphate
  • Organophosphates