Ligand-gated Ion Channels
Ligand-gated ion channels are a large group of intrinsic transmembrane proteins that allow passage of ions upon activation by a specific chemical. Most endogenous ligands bind to a site distinct from the ion conduction pore and binding directly causes opening or closing of the channel. Ligands can bind extracellularly, e.g. glutamate, ACh and GABA, or intracellularly, e.g. Ca2+ on Ca2+-activated potassium channels. It is important to note that the ligand itself is not transported across the membrane. Ligand binding causes a drastic change in the permeability of the channel to a specific ion or ions; effectively no ions can pass through the channel when it is inactive but up to 107 ions per second can be allowed through upon ligand binding.
Ligand-gated Ion Channel Target Files
Multiple diseases arise from abnormal functioning of ligand-gated ion channels. For example, overactivation of NMDA glutamate receptors allows Ca2+ entry, leading to activation of the apoptotic pathway and neurotoxicity - a process that may play a part in many neurodegenerative disorders.
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Potent, selective LRRK2 inhibitor
Tocris is the first to launch GSK2578215A, licensed from GlaxoSmithKline, for the study of Parkinson's Disease.