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. 2010 Spring;10(1):2-7.

G protein-coupled receptors as disease targets: emerging paradigms

Julia L Cook  1
Affiliations

G protein-coupled receptors as disease targets: emerging paradigms

Julia L Cook. Ochsner J. 2010 Spring.
No abstract available

Keywords: GPCR; RIP (regulated intramembrane proteolysis); nuclear receptors; receptor cleavage.

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Figures

Figure 1
Figure 1
Rat AT1 GPCR as it is oriented in the plasma membrane.
Figure 2
Figure 2
GPCRs can continue to signal following internalization. Following arrestin-mediated internalization, the AT1R can continue to signal through both ERK and JNK3 scaffolds, which permit phosphorylation activation of proteins downstream in the signaling pathways.
Figure 3
Figure 3
Fusion protein of the AT1R. The rat AT1R is fused in frame to upstream CFP and to downstream YFP. Fluorescent labels permit tracking and localization of proteins by fluorescent image digital capture.
Figure 4
Figure 4
Cleavage of the AT1R. Vascular smooth muscle cells were transfected with a construct encoding the AT1R labeled at the amino terminus with CFP (blue) and at the carboxy terminus with YFP (yellow). Three-dimensional deconvolution microscopy was performed on live cells at 24 hours after transfection. A. Cells were treated with vehicle, no ligand (cleavage was not induced). (i) YFP filter image. (ii) CFP filter image. (iii) Merged images from i and ii. Colocalization of fluors produces an aqua color. B. Cells were treated with 10−8 mol/L of Ang II for 1 hour before imaging. (i) YFP filter image. Note the presence of YFP in the nucleus and nuclear membrane (arrows). (ii) CFP filter image. Note the loss of cyan fluorescence from the cell perimeter (arrows). (iii) Merged images from i and ii.
See this image and copyright information in PMC

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