CRIM 2653 Lecture 42: V-GATED ION CHANNELS
23 May 2020
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Document Summary
8. 1) hts application to ion channels (most info presented here is for. Until recently, using voltage-gated ion channels as drug targets was difficult because of the limitations of relevant assay technologies traditional electrophysiology uses methods such as the single-cell patch clamp (the. Gold standard") -> which is labour intensive and of low-throughput nature. Advancements have allowed for non-electrophysiological, functional assay formats suitable for hts. Examples of these formats are : ion flux, ion-binding and voltage-sensitive dies: voltage-sensitive dye -> change optical properties with change in membrane potential, may be easier to apply to hts than automatizing the patch clamp technique. Advantages: useful for screening sizable compound libraries (typical in pharma industry), fewer associated costs, better speed. Disadvantages: (compared to gold standard) -> lack precision, temporal resolution, and voltage control, and may give many false positives (indirect read-out of channel activity)
