Thrombin receptor-activating peptides (TRAPs): Investigation of bioactive conformations via structure–activity, spectroscopic, and computational studies

…, P Andrade-Gordon, MF Addo, RM Scarborough…

Index: Ceruso, Marco A.; McComsey, David F.; Leo, Gregory C.; Andrade-Gordon, Patricia; Addo, Michael F.; Scarborough, Robert M.; Oksenberg, Donna; Maryanoff, Bruce E. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 11 p. 2353 - 2371

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Citation Number: 33

Abstract

The thrombin receptor (PAR-1) is an unusual transmembrane G-protein coupled receptor in that it is activated by serine protease cleavage of its extracellular N-terminus to expose an agonist peptide ligand, which is tethered to the receptor itself. Synthetic peptides containing the agonist motif, such as SFLLRN for human PAR-1, are capable of causing full receptor activation. We have probed the possible bioactive conformations of thrombin receptor- ...