Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule.

@article{Gadek2002GenerationOA,
  title={Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule.},
  author={Thomas R Gadek and D. J. Burdick and Robert S. McDowell and Michele S. Stanley and J. C. Marsters and Kristie J. Paris and David Oare and Mark R. Ter Molen Evan M. Tager Sarah E. Reynolds and Carol L. Ladner and K A Zioncheck and Wyne P Lee and Peter Gribling and Mark S. Dennis and Nicholas J. Skelton and Daniel B. Tumas and Kevin J. R. Clark and Susan M. Keating and Maureen H. Beresini and Jefferson W Tilley and Leonard G. Presta and Sarah C Bodary},
  journal={Science},
  year={2002},
  volume={295 5557},
  pages={1086-9}
}
The protein-protein interaction between leukocyte functional antigen-1 (LFA-1) and intercellular adhesion molecule-1 (ICAM-1) is critical to lymphocyte and immune system function. Here, we report on the transfer of the contiguous, nonlinear epitope of ICAM-1, responsible for its association with LFA-1, to a small-molecule framework. These LFA-1 antagonists bound LFA-1, blocked binding of ICAM-1, and inhibited a mixed lymphocyte reaction (MLR) with potency significantly greater than that of… CONTINUE READING
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