Nonspanning bivalent ligands as improved surface receptor binding inhibitors of the cholera toxin B pentamer.

@article{Pickens2004NonspanningBL,
  title={Nonspanning bivalent ligands as improved surface receptor binding inhibitors of the cholera toxin B pentamer.},
  author={Jason C. Pickens and Daniel D Mitchell and Jiyun Liu and Xiaojian Tan and Zhongsheng Zhang and Christophe L. M. Verlinde and Wim G. J. Hol and Erkang Fan},
  journal={Chemistry & biology},
  year={2004},
  volume={11 9},
  pages={
          1205-15
        }
}
  • Jason C. Pickens, Daniel D Mitchell, +5 authors Erkang Fan
  • Published in Chemistry & biology 2004
  • Chemistry, Medicine
  • A series of bivalent ligands of varying length were synthesized to inhibit the receptor-binding process of cholera toxin. Competitive surface receptor binding assays showed that significant potency gains relative to the constituent monovalent ligands were achieved independently from the ability of the extended bivalent ligands to span binding sites within the toxin pentamer. Several models that could account for the unexpected improvement in IC(50) values are examined, taking into account… CONTINUE READING

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