Michne W F, Schroeder J D
Department of Medicinal Chemistry, Sterling Winthrop Pharmaceuticals Research Division, Collegeville, Pennsylvania, USA.
Int J Pept Protein Res. 1996 Jan-Feb;47(1-2):2-8. doi: 10.1111/j.1399-3011.1996.tb00803.x.
The binding of lymphocyte function associated antigen (LFA-1) to intercellular adhesion molecule (ICAM-1) is responsible for several types of cellular adhesion. Amino-acid substitution mutants of ICAM-1 have established the importance of several sequences in this protein. We selected the binding region of Glu34 for further study. One published model of domain 1 placed Glu34 near the end of a beta-strand. We designed and synthesized three tripeptide derivatives centered on the Glu34 sequence and attached a platform which, through hydrogen bonds, induces a rigid beta-strand conformation. Variable temperature NMR methods coupled with NOESY 2D NMR data enabled determination of the solution conformation of these compounds.
