GPCR activation

Forfatter/Opretter:

Repapetilto

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beskrivelse:

Cartoon of GPCR Conformational Activation. Ligand binding disrupts an ionic lock between the E/DRY motif of TM-3 and acidic residues of TM-6. As a result the GPCR reorganizes to allow activation of G-alpha proteins. The side perspective is a view from above and to the side of the GPCR as it is set in the plasma membrane (the membrane lipids have been omitted for clarity). The intracellular perspective shows the view looking up at the plasma membrane from inside the cell. Based on information found in Mol. Endocrinol. 2010 24:261-274

Abbreviations, etc:

GPCR domains:

IL-1 to IL-3= Intracellular loops 1-3

EL-1 to EL-3= Extracellular loops 1-3

Other:

G-alpha= Alpha subunit of a heterotrimeric G-protein

G-beta/gamma= G-beta/gamma heterodimer of heterotrimeric G-protein

The figure is based on information found in the review article "The Year In G Protein-Coupled Receptor Research" Molecular Endocrinology 24 (1): 261-274. (2010)

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