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. Author manuscript; available in PMC: 2018 Jul 1.
Published in final edited form as: J Cardiovasc Pharmacol. 2017 Jul;70(1):10–15. doi: 10.1097/FJC.0000000000000475

Figure 1. GPCR signaling and desensitization.

Figure 1

Activation of GPCRs begins with binding of an agonist to the receptor. This leads to the exchange of GDP for GTP within the G protein α subunit followed by dissociation of the βγ subunit. These G proteins can then activate downstream effectors leading to various signaling pathways. GPCR signaling is halted via phosphorylation of the receptor by GRK, which then leads to internalization of the receptor through β-arrestin.