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Schering-Plough Research Institute, Kenilworth, NJ 07033
A thrombin receptor-radioligand binding assay was developed using
[3H]A(pF-F)R(ChA)(hR)Y-NH2
([3H]haTRAP), a high affinity thrombin
receptor-activating peptide (TRAP), and human platelet membranes.
Scatchard analysis of saturation binding data indicated that
[3H]haTRAP bound to platelet membranes with a
Kd of 15 nM and
a Bmax of 5.2 pmol/mg of protein. The
binding was reduced by GPPNHP, a nonmetabolizable GTP analogue. Various
TRAPs and a TRAP antagonist, but not other receptor agonists, displaced [3H]haTRAP from the binding sites.
SFLLRN-NH2, a thrombin receptor-tethered ligand analogue,
and [3H]haTRAP exhibited competitive binding for the same
binding sites. The relative affinity of these peptides for the binding
site paralleled their EC50 or IC50 values for
platelet aggregation. These data indicate that [3H]haTRAP
binds specifically and saturably to the functioning G protein-linked
thrombin (tethered ligand) receptor in human platelet membranes.
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