Ion transporters are membrane proteins that facilitate the passage of ions against their concentration gradients. They are significant drug targets that have broad implications in drug discovery and development. The ion flux of transporters is much lower than what would be observed in the case of ion channels and in some cases is non-existent. This makes study by conventional means quite difficult. Over the past few years, we have worked diligently to refine our assays to be able to screen compound libraries and perform structure-function assessments of ion transporters.
High throughput screening of NKCC1 Modulators (Roche) – NKCC1 transporters produce an electroneutral flux across cell membranes, making study by patch clamp impractical. A recent study published in conjunction with Roche details the ICR as a highly effective tool for high throughput screening of NKCC1 channels. As a result of this study, several hits were obtained from a focused library of 1450 compounds.
Researchers from Roche performed high-throughput screening campaigns for modulators of a cation-chloride co-transporter using the ICR 12000.
Download their poster from the 2016 Ion Channel Summit to see how Roche developed a high throughput rubidium (Rb+) uptake assay for measuring NKCC1 function and subsequently screened 1.2 million compounds using Aurora’s ICR 12000.