DEFINITION
After agonist binding and phosphorylation, many GPCRs — including GLP-1R — recruit β-arrestin and are internalised into clathrin-coated pits and endosomes. Internalised receptors may be recycled back to the plasma membrane, sorted for degradation, or continue to signal from endosomal compartments.
The kinetics and trafficking fate of internalised receptors are a major determinant of sustained agonist effect versus desensitisation.
WHY IT MATTERS
Receptor internalisation shapes the duration and character of GLP-1R signalling under sustained agonism.
RELATED
Compounds