| Autor: |
Carolin, Gerbeth-Kreul, Antje, Pommereau, Sven, Ruf, John L, Kane, Theresa, Kuntzweiler, Gerhard, Hessler, Christian K, Engel, Patrick, Shum, LinLi, Wei, Joerg, Czech, Thomas, Licher |
| Rok vydání: |
2021 |
| Předmět: |
|
| Zdroj: |
SLAS discovery : advancing life sciences RD. 26(6) |
| ISSN: |
2472-5560 |
| Popis: |
Classical high-throughput screening (HTS) technologies for the analysis of ionic currents across biological membranes can be performed using fluorescence-based, radioactive, and mass spectrometry (MS)-based uptake assays. These assays provide rapid results for pharmacological HTS, but the underlying, indirect analytical character of these assays can be linked to high false-positive hit rates. Thus, orthogonal and secondary assays using more biological target-based technologies are indispensable for further compound validation and optimization. Direct assay technologies for transporter proteins are electrophysiology-based, but are also complex, time-consuming, and not well applicable for automated profiling purposes. In contrast to conventional patch clamp systems, solid supported membrane (SSM)-based electrophysiology is a sensitive, membrane-based method for transporter analysis, and current technical developments target the demand for automated, accelerated, and sensitive assays for transporter-directed compound screening. In this study, the suitability of the SSM-based technique for pharmacological compound identification and optimization was evaluated performing cell-free SSM-based measurements with the electrogenic amino acid transporter B |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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