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@ARTICLE{Prescher:119829,
      author       = {H. Prescher and M. Frank$^*$ and S. Gütgemann and E.
                      Kuhfeldt and A. Schweizer and L. Nitschke and C. Watzl and
                      R. Brossmer},
      title        = {{D}esign, {S}ynthesis, and {B}iological {E}valuation of
                      {S}mall, {H}igh-{A}ffinity {S}iglec-7 {L}igands: {T}oward
                      {N}ovel {I}nhibitors of {C}ancer {I}mmune {E}vasion.},
      journal      = {Journal of medicinal chemistry},
      volume       = {60},
      number       = {3},
      issn         = {1520-4804},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2017-00424},
      pages        = {941 - 956},
      year         = {2017},
      abstract     = {Natural killer cells are able to directly lyse tumor cells,
                      thereby participating in the immune surveillance against
                      cancer. Unfortunately, many cancer cells use immune evasion
                      strategies to avoid their eradication by the immune system.
                      A prominent escape strategy of malignant cells is to
                      camouflage themselves with Siglec-7 ligands, thereby
                      recruiting the inhibitory receptor Siglec-7 expressed on the
                      NK cell surface which subsequently inhibits NK-cell-mediated
                      lysis. Here we describe the synthesis and evaluation of the
                      first, high-affinity low molecular weight Siglec-7 ligands
                      to interfere with cancer cell immune evasion. The compounds
                      are Sialic acid derivatives and bind with low micromolar Kd
                      values to Siglec-7. They display up to a 5000-fold enhanced
                      affinity over the unmodified sialic acid scaffold αMe
                      Neu5Ac, the smallest known natural Siglec-7 ligand. Our
                      results provide a novel immuno-oncology strategy employing
                      natural immunity in the fight against cancers, in particular
                      blocking Siglec-7 with low molecular weight compounds.},
      cin          = {W160},
      ddc          = {540},
      cid          = {I:(DE-He78)W160-20160331},
      pnm          = {314 - Tumor immunology (POF3-314)},
      pid          = {G:(DE-HGF)POF3-314},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:28103033},
      doi          = {10.1021/acs.jmedchem.6b01111},
      url          = {https://inrepo02.dkfz.de/record/119829},
}