KvLQT2
Kv7.2 is a voltage- and Lipid-gated [ion channels|lipid-gated] potassium channel protein coded for by the gene KCNQ2.
Mutations in the KCNQ2 gene are dominant autosomally inherited causes of benign familial [neonatal epilepsy].
Function
The M channel is a slowly activating and deactivating potassium channel that plays a critical role in the regulation of neuronal excitability. The M channel is formed by the association of the protein encoded by this gene and a related protein encoded by the KCNQ3 gene, both integral membrane proteins. M channel currents are inhibited by M1 muscarinic acetylcholine receptors and activated by retigabine, a novel anti-convulsant drug. Defects in this gene are a cause of benign familial neonatal convulsions type 1, also known as epilepsy, benign neonatal type 1. At least five transcript variants encoding five different isoforms have been found for this gene.Ligands
- ICA-069673: channel opener at KCNQ2/Q3, 20-fold selective over KCNQ3/Q5, no measurable activity against a panel of cardiac ion channels and no activity on GABAA gated channels at 10 μM. A range of related benzamides exhibited activity, of which compound number 40 is shown here.
- ML252: channel inhibitor, IC50 = 70nM.
- Phosphatidylinositol 4,5-bisphosphate