Reliable, high throughput KV7 assays are important because KV7 ion channels play a key role in regulating neuronal excitability, which is closely linked to both pain signalling and seizure activity.
Reliable, high throughput KV7 assays are important because KV7 ion channels play a key role in regulating neuronal excitability, which is closely linked to both pain signalling and seizure activity.
Understanding cardiac safety early is critical in drug development. In their latest poster, Jazz Pharmaceuticals, explain how they utilised Metrion’s clinically translatable cardiotoxicity assay to do exactly that.
Aligos Therapeutics and Metrion explore key approaches to cardiovascular safety screening in drug discovery.
We developed a high-throughput, electrophysiological assay of TREK-1 function to identify novel modulators. The assay was optimized to identify both activators and inhibitors, providing comprehensive mechanistic data for high value, limited supply screening libraries, such as the venom fraction library used in this study (Targeted Venom Discovery Array, T-VDA, Venomtech, UK).
Kv7 ion channels are highly relevant to epilepsy because they are voltage gated potassium ion channels that help regulate neuronal excitability and suppress excessive electrical firing in the brain.
Cardiac toxicity remains the leading cause of new drug safety side-effects. Current preclinical cardiac safety assays rely on in vitro cell-based ion channel assays and ex vivo and in vivo animal models⁽¹⁾. These assays provide an indication of acute risk but they do not always predict the effect of chronic compound exposure, as recently seen with oncology drugs. Therefore, new assays are required to characterise chronic structural and functional effects in human cells earlier in drug discovery. Impedance-based technology can provide more accurate chronic cardiotoxicity measurements in an efficient manner using human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs).
By accurately defining the drug exposure levels that affect QRS duration, researchers can establish safety margins, prioritise lower-risk compounds, and reduce the chance of late-stage failures due to cardiac toxicity
We demonstrate the generation and validation of a stable CHO-hHCN2 cell line used as a cellular tool in the successful development of hHCN2 automated electrophysiology screening assays.
Kv7 channels are a family of voltage gated potassium ion channels that play a key role in controlling cellular excitability.
Metrion and Sophion collaborated to determine whether other insoluble salts can act as seal enhancers, or whether this property is unique to CaF2.