Drug Discovery 2017
Poster
38

Targeting Transporters with HTS Electrophysiology on the SURFE2R 96SE.

Objective

Due to the growing interest in membrane transporters as drug targets there is an increasing demand for efficient, reliable and flexible systems for measuring transporter activity. Solid Supported Membrane (SSM)-based electrophysiology has emerged as a promising technique for the biophysical and pharmacological characterization of electrogenic membrane proteins. SSM-based electrophysiology is a label-free measuring method which allows the use of reconstituted protein or membrane samples from native tissues or cell culture. The technique is highly sensitive and enables the resolution of low turnover transport and even binding- events, which may not be detectable using conventional electrophysiological methods. The technique was invented in the 90’s and since its introduction, more than 100 different proteins have been tested. However, the method is still under-utilized primarily due to its limited throughput. Here we present a novel high throughput instrument for SSM measurements recording from 96 samples simultaneously. Data is presented showing several different targets including SLC transporters, the neuronal glutamate transporter, EAAT3, the organic cation transporter, OCT2, the Na+/Ca2+ exchanger, the Na+/K+-ATPas and the nicotinic acetylcholine receptor (nAChR). Overall, we demonstrate that the SURFE2R 96SE is a novel, high throughput and flexible tool for transporter research and drug discovery.

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ELRIG

The European Laboratory Research & Innovation Group Our Vision : To provide outstanding, leading edge knowledge to the life sciences community on an open access basis

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