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. Author manuscript; available in PMC: 2012 Dec 10.
Published in final edited form as: Exp Cell Res. 2011 Oct 6;317(20):2981–2994. doi: 10.1016/j.yexcr.2011.10.001

Figure 8. Hypothetical model of GR internalization.

Figure 8

Upon ligand binding, GRs are desensitized and targeted for internalization through either a clathrin-mediated pathway or through caveolae. The internalization involves β-arrestins, which colocalize with the receptors at the membrane and intracellularly. The internalized receptors rapidly enter early endosomes. Second messengers GRK2, GRK3 and GRK5 as well as PKCα stimulate receptor internalization. Abbreviations: G, glucagon; GR, glucagon receptor; AR, β-arrestins; CCP, clathrin coated pit; CCV, clathrin-coated vesicle; EE, early endosome; CAV, caveolae; CS, caveosome; GRK, G protein-coupled receptor kinase; PAO, phenylarsine oxide; N, nucleus; DN, dominant negative.