G Protein-Gated Ion Channel
G protein-gated ion channels are a family of transmembrane ion channels in neurons and atrial muscle cells, which are directly controlled by G protein. G protein-gated ion channels affect the flow of potassium (K⁺), calcium (Ca2⁺), sodium (Na⁺) and chloride (Cl-) across the plasma membrane.
Generally, G protein-gated ion channels are specific ion channels located in the plasma membrane of cells, which are directly activated by a series of related proteins. Ion channels allow certain ions to move selectively across the plasma membrane in the cell. More specifically, in nerve cells, together with ion transporters, they are responsible for maintaining the electrochemical gradient across the cell.
G protein-gated ion channels are associated with specific types of G protein-coupled receptors. G protein is a family of intracellular proteins that can mediate signal transduction pathways. Each G protein is a heterotrimer of three subunits: α-, β- and γ-subunits. The receptor protein has a large extracellular binding domain, which will bind to its respective ligands (such as neurotransmitters and hormones). Once the ligand binds to its receptor, a conformational change occurs. This conformational change of the G protein allows Gα to bind to GTP. Different types of G protein-coupled receptors have many known functions, including cAMP and phosphatidylinositol signal transduction pathways. A class of receptors called metabotropic glutamate receptors play an important role in the activation of G protein indirect ion channels. These pathways are activated by second messengers, which trigger a signal cascade involving various proteins that are important for the cell's response.
Fig.1 G protein-gated ion channel.
Clinical Significance
G protein mutations associated with G protein-gated ion channels have been shown to be associated with diseases such as epilepsy, muscle diseases, neurological diseases, and chronic pain.
Epilepsy, chronic pain and addictive drugs such as cocaine, opioids, cannabinoids and ethanol can affect neuronal excitability and heart rate. Gated inwardly-rectifying potassium (GIRK) channels have been shown to be associated with seizure susceptibility, cocaine addiction, and increased tolerance to opioids, cannabinoids, and ethanol. This connection suggests that GIRK channel modulators may be useful therapeutic agents for the treatment of these diseases. GIRK channel inhibitors can be used to treat cocaine, opioid, cannabinoid and ethanol addiction, while GIRK channel activators can be used to treat withdrawal symptoms.
The research of G protein-gated ion channels requires a series of scientific research products. Creative Biolabs has been devoted to the research and development of the most advanced reagents to assist ion channel research. Our product portfolio covers a complete list of GPCR activators and blockers, monoclonal antibodies, labeled antibodies, proteins and assay kits.
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