2. Academic Validation
  3. Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000

Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000

  • J Med Chem. 2009 Aug 13;52(15):4960-3. doi: 10.1021/jm900290r.
Vivien Lacône 1,  Julie Hunault,  Muriel Pipelier,  Virginie Blot,  Thomas Lecourt,  Jézabelle Rocher,  Anne-Laure Turcot-Dubois,  Séverine Marionneau,  Jean-Yves Douillard,  Monique Clément,  Jacques Le Pendu,  Marc Bonneville,  Laurent Micouin,  Didier Dubreuil
Affiliations

Affiliation

  • 1 Université de Nantes, CNRS, Chimie et Interdisciplinarité: Synthèse, Analyse, Modélisation (CEISAM), UMR CNRS 6230, Faculté des Sciences et des Techniques, 2 Rue de la Houssinière, BP 92208, 44322 Nantes Cedex 3, France.
PMID: 19580320 DOI: 10.1021/jm900290r
Abstract

4-Deoxy-alpha-GalCer analogues are considered weaker agonists than KRN7000 for the stimulation of human iNKT cells, but this remains strongly debated. In this work, we described a strategy toward 4-deoxy-alpha-GalCers with, as a key step, a metathesis reaction allowing sphingosine modifications from a single ethylenic alpha-galactoside precursor. The 4-deoxy-KRN7000 derivative 2, described here, induced potent cytokinic responses, comparable to those of KRN7000, both from human iNKT cells in vitro and from their murine counterpart in vivo.

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