Ion channels and membrane proteins

Ion channels and membrane proteins represent a broad category of biological molecules that reside within the lipid bilayer of cells and organelles, serving as the primary interface between the cell and its environment (Santos et al., 2017, Nature Reviews Drug Discovery). This group includes voltage-gated and ligand-gated ion channels, G protein-coupled receptors (GPCRs), and various solute carriers and ATP-dependent transporters (Overington et al., 2006, Nature Reviews Drug Discovery). They are essential for maintaining cellular homeostasis, generating action potentials in excitable tissues, and facilitating the transport of nutrients and waste (Bagal et al., 2013, Journal of Medicinal Chemistry). Due to their critical physiological roles and accessibility to extracellular drugs, they account for approximately 60% of all current therapeutic targets (Santos et al., 2017). Dysfunctions in these proteins are implicated in a wide range of pathologies, including cardiac arrhythmias, epilepsy, cystic fibrosis, and various cancers (StatPearls, 2023, Ion Channels). Pharmacological agents targeting these proteins include a diverse array of small molecules and biologics that modulate their activity to treat chronic and acute conditions.

Other names

Integral membrane proteinsTransmembrane proteinsSurface proteinsMembrane-bound proteins

Drugs targeting these proteins typically act as pore blockers, allosteric modulators, competitive antagonists, or agonists to regulate the movement of ions and molecules or to initiate intracellular signaling cascades.