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. 2002 Feb 8;295(5557):1086-9.
doi: 10.1126/science.295.5557.1086.

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

T R Gadek  1 , D J Burdick, R S McDowell, M S Stanley, J C Marsters Jr, K J Paris, D A Oare, M E Reynolds, C Ladner, K A Zioncheck, W P Lee, P Gribling, M S Dennis, N J Skelton, D B Tumas, K R Clark, S M Keating, M H Beresini, J W Tilley, L G Presta, S C Bodary
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Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule

T R Gadek et al. Science. .

VSports最新版本 - Abstract

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 cyclosporine A. Furthermore, in comparison to an antibody to LFA-1, they exhibited significant anti-inflammatory effects in vivo. These results demonstrate the utility of small-molecule mimics of nonlinear protein epitopes and the protein epitopes themselves as leads in the identification of novel pharmaceutical agents VSports手机版. .

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