ML297 (VU0456810), GIRK activator

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

GIRK2 also known as KCNJ5 or H-ERG is a potassium channel protein. It conducts potassium ions across cell membranes assisting in the regulation of electrical activity within cells. GIRK2 consists of subunits that form a channel with a mass of approximately 53 kDa. This protein expresses mainly in the brain heart and pancreas playing significant roles in each of these tissues.

Biological function summary

GIRK2 contributes to maintaining the resting membrane potential and modulating neuronal excitability. It forms part of a larger complex by interacting with other proteins such as GIRK1 which aids in its regulation and function. Its activity is primarily modulated by G-proteins which enable it to participate in responding to various cellular signals affecting excitation and inhibition balance within neurons.

Pathways

GIRK2 plays a significant role within the G-protein-coupled receptor (GPCR) signaling pathway. In heart tissue GIRK channels contribute to the parasympathetic regulation of the heart rate by the acetylcholine muscarinic receptors. Furthermore GIRK2 interacts with various signaling molecules like the beta-gamma subunits of G-proteins which modulates the activity of the potassium channel in response to neurotransmitter signals.

GIRK2 has associations with disorders such as cardiac arrhythmias and neuropsychiatric disorders. Mutations or dysregulation in GIRK2 can lead to Long QT Syndrome a cardiac condition related to its role in cardiac repolarization. Its relation to neuropsychiatric disorders stems from its function in the brain where it interacts with proteins like GIRK1 and other ion channels influencing neural health and activity.