Research Topic

Structure Related Druggability of Voltage-gated Sodium and Calcium Ion-Channels to treat diseases

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About this Research Topic

Voltage-gated ion channels play crucial roles in both excitable and non-excitable cells. Therefore, they constitute interesting drug targets. About 15% of the drugs used to treat human diseases target ion channels. High blood pressure Ca2+ channel blockers, antiarrhythmics, antiepileptics, and local ...

Voltage-gated ion channels play crucial roles in both excitable and non-excitable cells. Therefore, they constitute interesting drug targets. About 15% of the drugs used to treat human diseases target ion channels. High blood pressure Ca2+ channel blockers, antiarrhythmics, antiepileptics, and local anesthetics, are all examples of drugs that target voltage-gated ion channels. The majority of these drugs use the same mechanism in inhibiting ion channels’ activity, which is blocking the central pore. A small number of drugs target other areas of the channels and allosterically enhance the collapse of the pore.

The main disadvantage of pore blocker drugs that target voltage-gated sodium and calcium channels is that they are not specific for one type of voltage-gated ion channels. This may engender serious side effects that sometimes can be fatal. If we can develop a drug that specifically targets one type of a voltage-gated ion channel with high specificity and low toxicity that would be beneficial to patients who suffer from drugs’-side effects. This Topic will shed the light on the subtle structural differences between different types of voltage-gated sodium and calcium channels, which could be used as a marker to target one subtype of each ion channel. It will also help medicinal chemists, biophysicists, and structural biologists interested in structure-based drug design to use these differences into their considerations during the rational drug design process.

The aim of this Research Topic is to develop articles focused on discussing the potential druggability of each structural component of the voltage-gated sodium and calcium ion channels. We invite authors to contribute Original Research articles, Review and Mini Reviews focused on voltage-sensing domain as a potential drug target, as well as articles focusing on the pore domain or the fenestrations as a potential drug targets. These different structures of a voltage-gated ion channel will be discussed in the light of its current or prospective role as a drug target.

Themes covered by this Research Topic include:
• Structural differences between voltage-gated sodium channels.
• Structural differences between voltage-gated calcium channels.
• Druggability of the voltage-sensing domain of voltage-gated sodium and calcium channels.
• Druggability of the pore domain and fenestrations of voltage-gated sodium and calcium channels.


Keywords: Voltage-gated, Ion-channels, Druggability, Calcium, Sodium


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