DISCOVER Bioactive Small Molecules for Ion Channels Research

Ion transport across the relatively impermeable lipid bilayer of the cell membrane is accomplished via membrane proteins known as ion channels, pumps and transporters. Ion channels are gated pores and may open and close either intrinsically or in response to regulators such as chemical ligands or changes in membrane voltage gradients; they are found in the membranes of virtually all types of plant, animal and bacterial cells. Ion channels regulate passage of ions like calcium, chloride, sodium, and potassium through cell membranes, in and out of cell organelles, and play a role in cell signaling. Hundreds of ion channels have been identified and many are classified based on characteristics such as gating (e.g. ligand-gated, voltage-gated) and type of ion that passes through the channel; other, smaller categories, also exist.

  • Calcium channels - At least six classes of voltage-gated calcium channels serve as the major route of calcium translocation across the plasma membrane. The channels support functions such as muscle contraction, hormone and neurotransmitter release, cell motility, cell growth and regulation, cell damage and death, and cell survival.

  • Chloride channels - Several different types show different regulatory characteristics, but all are involved in chloride conductance. In cells, chloride channels have been shown to be involved in pH regulation, cell volume regulation, and organic solute transport.

  • HCN channels - Gated by voltage as well as direct activation by cyclic nucleotides. HCN channels play a central role in initiation and control of the heart beat, and support multiple brain functions such as sleep-wake cycle, motor learning, and dendritic signal integration.

  • Potassium channels - Integral membrane proteins that allow selective, diffusional passage of potassium ions across biological membranes. Potassium channels are essential for control of membrane potential, regulation of cell volume, and secretion of salt, neurotransmitters, and hormones.

  • Epithelial sodium channels (ENaC) - Constitutively active channel that mediates Na+ transport, which is important for control of Na+ and K+ homeostasis and blood pressure in the kidney and colon, keeping the composition and volume of luminal fluid constant.

  • Sodium channels - Voltage-gated sodium channels are pres­ent in most excitable cell membranes and play an important role in generating action potentials.

  • Transient receptor potential (TRP) channels - Group of ion channels that are relatively non-selectively permeable to cations. TRP channels can be gated by G protein-couple receptor (GPCR) signaling, lipids, ions, osmolarity, voltage or even hot or cold temperatures.

Given the important roles that they plan in a wide variety of biological processes, it is not surprising that disruption of normal function of ion channels has been associated with a number of diseases, including cardiac disrhythmia, hypertension, neuropathic pain syndromes, epilepsy, and cystic fibrosis. The involvement of ion channels in disease makes them Important potential targets. Sigma® Life Science understands that it is essential to ensure that your target is the right target in order to translate basic understanding of ion channels into therapeutic treatments. Sigma offers several inhibitors, agonists and antagonists for target identification and validation in ion channel research; a selection of these research tools is shown below.


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