GIRK

G protein-gated Kir Channels (Kir3.x, a.k.a. KG channels or GIRKs) are one of the targets of GPCRs, that, upon activation of the GPCR by its ligand (hormone or neurotransmitter) release two intracellular effector molecules (Gα and Gβγ) that can effectuate channel opening resulting in hyperpolarization of the cell. The KG channels can be activated by intracellular GTP (GTPi) in the presence of agonist or by intracellular GTPγS even in the absence of agonist. After a long controversy, it was finally established that KG channels are activated by Gβγ subunits of PTX-sensitive G proteins. Functional KG channels are tetrameric assemblies of Kir3 family subunits and can be either homomeric or heteromeric. The composition of subunit of KG channels varies among different cells and tissues which allows them to play diverse functional roles[1].


[1] H. Hibino et al. Inwardly rectifying potassium channels: their structure, function, and physiological roles. Physiol Rev. 2010 Jan;90(1):291-366.

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2436 ML 297 First potent and selective activator of the GIRK potassium channel €95.00

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