English: Cartoon depicting the GPCR-G-protein activation/deactivation cycle. In the resting state the receptor may be found associated with a heterotrimeric G-protein with GDP bound to its alpha subunit. Agonist binding to the GPCR induces a cascade of conformational changes first in the receptor and then in the bound G-alpha subunit of the G-protein. This results in release of GDP which is soon replaced by GTP. The cell maintains a 10:1 ratio of cytosolic GTP:GDP so exchange for GTP is ensured. GTP-bound G-alpha takes yet another conformation that has low affinity for the GPCR as well as the Beta-Gamma complex, so all three dissociate from one another. GTP-G-alpha and the G-beta/gamma complex then go on to allosterically modulate the activies of various downstream effector proteins, but diffusion is usually limited to the membrane surface due to the presence of palmitoyl and a GPI-anchor, respectively. The GTP-binding site of G-alpha is also capable of hydrolyzing GTP to GDP, albeit at a relatively slow rate. This rate can be increased by binding to various GTPase activating Proteins (GAPs) such as those of the RGS family. Many effector molecules modulated by G-alpha also have GAP activity. Upon GTP hydrolysis the G-alpha subunit is rendered inactive and once again may bind G-beta/gamma and form a heterotrimeric G-protein, which will often be found associated with an unliganded GPCR.
Abbreviations, etc:
GPCR= G-protein Coupled receptor
G-alpha= G-alpha subunit of a heterotrimeric G-protein
G-beta/gamma= Complex of G-beta-gamma subunits of a heterotrimeric G-protein
to share – to copy, distribute and transmit the work
to remix – to adapt the work
Under the following conditions:
attribution – You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
share alike – If you remix, transform, or build upon the material, you must distribute your contributions under the same or compatible license as the original.
Permission is granted to copy, distribute and/or modify this document under the terms of the GNU Free Documentation License, Version 1.2 or any later version published by the Free Software Foundation; with no Invariant Sections, no Front-Cover Texts, and no Back-Cover Texts. A copy of the license is included in the section entitled GNU Free Documentation License.http://www.gnu.org/copyleft/fdl.htmlGFDLGNU Free Documentation Licensetruetrue
You may select the license of your choice.
Captions
Add a one-line explanation of what this file represents
Items portrayed in this file
depicts
creator
some value
object of statement has role: photographer
author name string: Repapetilto
Wikimedia username: Repapetilto
copyright status
copyrighted
copyright license
GNU Free Documentation License, version 1.2 or later
minor edits. G-alpha is targeted to the membrane via palmitoylation not due to GPI-linkage. The C-terminal tail interacts with GPCRs so the original claim did not make sense.
{{Information |Description={{en|1=Cartoon depicting the GPCR-G-protein activation/deactivation cycle. In the resting state the receptor may be found associated with a heterotrimeric G-protein with GDP bound to its alpha subunit. Agonist binding to the GPC