Mechanism
The mechanism of homologous desensitization is as follows (using the β2 receptor as an example):
- Agonist binds and activates receptor which changes to an active conformational state.
- Beta adrenergic receptor kinase (BARK), a cytoplasmic kinase is activated and phosphorylates the C-terminus of the β2 receptor.
- Such phosphorylation increases the affinity of β-arrestin for the receptor, resulting in uncoupling of the α subunit of the heterotrimeric G-protein from the receptor producing desensitization.
Read more about this topic: Homologous Desensitization
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