Ion Channels

Ion channels are pore-forming membrane proteins which allow the flow of ions to pass through the membranes. The activity of ion channels is the ability of cells to regulate the speed of the corresponding substances in and out of cells through the opening and closing of ion channels. Ion channels are key components in a wide variety of biological processes involving rapid changes in cells and are important for achieving various functions of the cell.

Because ion channels play a crucial role in controlling a very wide spectrum of physiological processes and their dysfunction can lead to pathophysiology, they are well recognized as important therapeutic targets for treating a number of different pathophysiologies. Ion channels have been common drug targets for various diseases, including cardiac disorders, kidney failure, neurological indications, the perception of pain and blindness. Abnormal structure or dysfunction of ion channels can cause channelopathy. Because of these, ion channels have become an attractive potential target class for drug discovery.

Cartoon representation of the basic structural components of an ion channel Figure 1. Cartoon representation of the basic structural components of an ion channel. (Bagal, S. K., et al., 2013)

Creative Biolabs provides a comprehensive target validation services to help confirm various ion channels as therapeutic targets of drug discovery process thus to deal with data reproducibility crisis which is a big obstacle for drug research and development and may lead to failure and high risk of investment.

Creative Biolabs provides a comprehensive list of assays on multiple high-quality platforms to characterize the features of different ion channels as your drug targets to advance your drug discovery. With experienced experts and cutting-edge technologies, we can provide high-quality and reliable services in a time-saving and cost-efficient manner. We offer professional target validation services for the following types of ion channels classified by gating.

Voltage-Gated Ion Channel

Voltage-gated ion channel (VDAC) is a class of transmembrane ion channel proteins that forming a gated, water-filled pore to control the flow of ions between the intracellular and extracellular environments. The open and close of VDAC are in response to changes in the membrane potential of cells. The membrane potential alters the conformation of the channel proteins. The main subfamilies of VDAC include voltage-gated sodium channels, voltage-gated calcium channels, voltage-gated potassium channels and voltage-gated proton channels.

Ligand-Gated Ion Channel

Ligand-gated ion channel (LGIC), also known as ionotropic receptor, is a class of transmembrane ion channel protein containing a pore that opens in response to specific ligand molecules binding to the extracellular domain of the receptor protein, allowing ions such as Na+, K+, Ca2+, and/or Cl- to pass through the membrane. Ligand binding leads to conformational changes in the structure of the channel proteins, which ultimately cause the opening of the channel gates and subsequent ion flux through the plasma membrane. The typical examples of LGIC are GABAA receptors, ionotropic glutamate receptors and 5-HT3 receptors.

Creative Biolabs has a dedicated assay development team that will work closely with you to design customized assays for your specific drug target. Our service will meet your specific needs fast at extremely competitive prices. If you need more information, please feel free to contact us at anytime. We look forward to working with you and helping your drug research and development project succeed.

Reference

  1. Bagal, S. K., et al., 2013. Ion channels as therapeutic targets: a drug discovery perspective. Journal of Medicinal Chemistry, 56(3), pp. 593-624.
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