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Issue 9, 2011
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The stimulating adventure of KRN 7000

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Associated with the CD1d protein, KRN 7000, a potent synthetic α-galactosylceramide, is known to activate the invariant NKT immune cells. This stimulation then leads to the production of different cytokines modulating a TH1/TH2 immune response balance involved in protection against several pathologies such as autoimmune diseases and cancers. Various efforts have been made toward the synthesis of simple and more functionalized analogues in order to selectively induce TH1 or TH2-type cytokine production. Since the discovery of KRN 7000, structure-activity relationships, crystallographic and modelling studies have pointed to the potential of several GalCer analogues in term of selective bioactivity, and have highlighted interesting elements in order to better understand the recognition and activation mechanisms of immune iNKT cells. By presenting an up-to-date library of analogues, collecting recent breakthroughs done in crystallography and molecular modelling, and relating them to the available biological results, we hope that this review will highlight and help the scientific community in their KRN research.

Graphical abstract: The stimulating adventure of KRN 7000

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Publication details

The article was received on 03 Nov 2010, accepted on 12 Jan 2011 and first published on 11 Mar 2011

Article type: Perspective
DOI: 10.1039/C0OB00975J
Citation: Org. Biomol. Chem., 2011,9, 3080-3104
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    The stimulating adventure of KRN 7000

    A. Banchet-Cadeddu, E. Hénon, M. Dauchez, J. Renault, F. Monneaux and A. Haudrechy, Org. Biomol. Chem., 2011, 9, 3080
    DOI: 10.1039/C0OB00975J

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