Chemistry

[ASAP] Altered Intracellular Trafficking as a Mechanism for Prolonged Duration of G Protein-Coupled Receptor Activation

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This study investigates how altered intracellular trafficking pathways can extend the duration of G protein-coupled receptor (GPCR) signaling beyond what occurs at the plasma membrane. The research demonstrates that GPCRs can continue to activate G protein-dependent signaling after internalization into endosomal compartments, with trafficking dynamics playing a key role in determining the overall temporal profile of receptor activity. These findings suggest that the spatial location of receptor signaling within the cell is a critical determinant of how long and how strongly a receptor response is sustained.


Understanding how intracellular trafficking modulates GPCR signaling duration has significant implications for drug development, as many therapeutic targets are GPCRs and designing ligands that influence receptor trafficking could offer more precise control over signaling outcomes and reduced side effects.


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Journal of the American Chemical Society
DOI: 10.1021/jacs.6c02192

Source: [ASAP] Altered Intracellular Trafficking as a Mechanism for Prolonged Duration of G Protein-Coupled Receptor Activation