Voltage- and ligand-gated ion channels and transporters

Voltage- and ligand-gated ion channels and transporters represent a vast and heterogeneous group of membrane proteins that regulate the flux of ions and molecules across cellular membranes. Voltage-gated channels are essential for generating and propagating action potentials in excitable tissues, while ligand-gated channels mediate rapid synaptic transmission in response to neurotransmitters (Alexander SP, et al., 2023). Transporters, including solute carriers and ATP-powered pumps, maintain cellular homeostasis by moving nutrients, ions, and waste products against or along concentration gradients (Purves D, et al., 2001). These proteins are foundational to human physiology, governing processes such as cardiac rhythm, sensory perception, and renal function. Consequently, they are among the most successful classes of therapeutic targets, with drugs acting as blockers, activators, or modulators to treat a wide spectrum of disorders including epilepsy, hypertension, and clinical depression (Yu FH, Catterall WA, 2004). Their ubiquitous expression, however, necessitates high selectivity to avoid systemic toxicities such as cardiotoxicity or neurotoxicity.

Other names

Ion channels and solute carriersMembrane transport proteinsElectrogenic pores and pumpsVoltage-gated ion channels (VGICs)Ligand-gated ion channels (LGICs)Solute carrier (SLC) transportersATP-binding cassette (ABC) transporters

Inhibition, activation, or allosteric modulation of ion flow or solute translocation across biological membranes.