Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates
Introduction. R-Thrombin is a key trypsin-like serine protease involved in coagulation and a variety of cellular actions, such as platelet aggregation, lymphocyte mitosis, monocyte chemotaxis, and endothelial cell proliferation. 1-4 Many of the effects of thrombin on cells are mediated by specific cell-surface receptors, which eluded identification for many years. However, in 1991, Coughlin and co-workers identified the first example of a thrombin ...
