4.6 Article

Second generation of fucose-based DC-SIGN ligands: affinity improvement and specificity versus Langerin

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 9, Issue 16, Pages 5778-5786

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05573a

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Funding

  1. FIRB program CHEM-PROFARMANET [RBPR05NWWC]
  2. Marie Curie ITN [PITN-GA-2008-213592]
  3. Comune di Milano [55/2008]

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DC-SIGN and Langerin are two C-type lectins involved in the initial steps of HIV infections: the former acts as a viral attachment factor and facilitates viral invasion of the immune system, the latter has a protective effect. Potential antiviral compounds targeted against DC-SIGN were synthesized using a common fucosylamide anchor. Their DC-SIGN affinity was tested by SPR and found to be similar to that of the natural ligand Lewis-X (Le(X)). The compounds were also found to be selective for DC-SIGN and to interact only weakly with Langerin. These molecules are potentially useful therapeutic tools against sexually transmitted HIV infection.

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