In a recent post on Venomous toxin ion channel modulators, we looked at toxin derived peptides to manipulate a wide variety of ion channels. These toxins can be used as tools to characterize specific ion channels, but they can also be utilized as reference inhibitors in ion channel drug screening campaigns.
Today, let’s take a look at cell lines over expressing specific ion channels and designed for cell based ion channel assays in drug discovery.
Ion channels are proteins with pore-forming abilities. Their selective capabilities to let ions cross the cell membrane involves them in crucial cellular functions (controlling membrane potential, the flow of ions, regulating cell volume). As ion channels are involved in the patho-physiology of so many diseases, they are natural candidates for pharma R&D programs.
To screen for ion channel inhibitors, cell lines are needed to expose functional ion channels to potential drug candidates. These cells lines have to stably express the ion channel of interest and should be characterized in terms of functionality of the respective channel.
Ion channel over expressing cell lines
BPS Biosciences have developed a set of cell lines with interesting targets for drug discovery campaigns. Most of these cell lines have been characterized with influx experiments.
They cover diverse ion channels classes, such as Calcium-, Potassium-, and Sodium-channels and others.
- CFTR – HEK 293 Cell Line: ABC transporter-class ion channel
- hTMEM16A – HEK293 Cell Line: Calcium-activated chloride channel
- hTRPC3 – HEK293 Cell Line: transient receptor potential channel (TRP) – Fig. 1 shows typical influx results obtained with this cell line using Fluo-8 as an indicator for Ca2+.
- IKCA1 (KCNN4) – HEK293 Cell Line: part of a potentially heterotetrameric voltage-independent potassium channel
- NaV1.7–HEK293 Cell Line: voltage-gated sodium ion channel
- Nav1.8/β2 – HEK293 Cell Line: voltage gated type X, alpha subunit sodium channel
- TMEM16B (ANO2) – HEK293 Recombinant Cell line: Calcium-activated chloride channel
- TRPC7-HEK293 Cell Line: transient receptor potential cation channel
- TRPM2-HEK293 Cell Line: transient receptor potential channel (TRP)
- hERG (Kv11.1) – HEK293 Recombinant Cell line: alpha subunit of a potassium ion channel, Kv11.1. Typical results of influx experiments are shown in Fig. 2.
- SLC5A5 – HEK293 Recombinant Cell line: sodium-dependent transporter of iodide
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