Receptors coupled with G proteins (GPCRs) control numerous cellular functions, but the intracellular interaction between receptors and G proteins has proved difficult to block specifically. In September 23
Using platelets Covic et al. observed that attachment of a palmitate lipid to peptides based on the third intracellular loop of protease-activated receptor 1 or 4 (PAR1, PAR4) yielded potent inhibitors of thrombin-mediated aggregation. In addition, they showed that infusion of the anti-PAR4 pepducin into mice extended bleeding time and protected against systemic platelet activation.
"The deployment of i3-loop pepducins provides a simple and powerful approach to determine the effect of pharmacological disruption of GPCRs that lack a known extracellular...