Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates

HC Zhang, CK Derian, P Andrade-Gordon…

Index: Zhang; Derian; Andrade-Gordon; Hoekstra; McComsey; White; Poulter; Addo; Cheung; Damiano; Oksenberg; Reynolds; Pandey; Scarborough; Maryanoff Journal of Medicinal Chemistry, 2001 , vol. 44, # 7 p. 1021 - 1024

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Citation Number: 87

Abstract

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 ...