A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes
Quynh N. Mai, Priyank A. Shenoy, Tim Quach, Jeffri S. Retamal, Arisbel B. Gondin, Holly R. Yeatman, Luigi Aurelio, Joshua Conner, Daniel P. Poole, Meritxell Canals, Cameron J. Nowell, Bim Graham, Thomas P. Davis, Stephen J. Briddon, Stephen J. Hill, Christopher J. H. Porter, Nigel W. Bunnett, Michelle L. Halls, Nicholas A. Veldhuis
Abstract
R antagonists is an important step toward understanding how we can effectively target intracellular GPCRs in disease.
Topics & Concepts
EndosomeInternalizationCell biologyTachykinin receptor 1G protein-coupled receptorEndocytosisReceptorSignal transductionArrestinCell signalingBiologyChemistrySubstance PBiochemistryIntracellularNeuropeptideReceptor Mechanisms and SignalingNeuropeptides and Animal PhysiologyPain Mechanisms and Treatments