[HTML][HTML] Rational optimization of a short human P-selectin-binding peptide leads to nanomolar affinity antagonists
CCM Appeldoorn, TJM Molenaar, A Bonnefoy… - Journal of Biological …, 2003 - ASBMB
P-selectin plays an important role in the development of various diseases, including
atherosclerosis and thrombosis. In our laboratory we recently identified a number of specific
human P-selectin-binding peptides containing a Glu-Trp-Val-Asp-Val consensus motif,
displaying a low micromolar affinity for P-selectin (IC 50= 2 μm). In search of more potent
antagonists for P-selectin, we have optimized the EWVDV pentapeptide core motif via a two-
step combinatorial chemistry approach. A dedicated library of peptide derivatives was …
atherosclerosis and thrombosis. In our laboratory we recently identified a number of specific
human P-selectin-binding peptides containing a Glu-Trp-Val-Asp-Val consensus motif,
displaying a low micromolar affinity for P-selectin (IC 50= 2 μm). In search of more potent
antagonists for P-selectin, we have optimized the EWVDV pentapeptide core motif via a two-
step combinatorial chemistry approach. A dedicated library of peptide derivatives was …