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Electrogenic proteins - such as ion channels, transporters and exchangers - have emerged as an attractive target class and several marketed drugs elicit their therapeutic effects through the modulation and interactions with these proteins.
The development of robust functional assays and useful devices for screening extensive collections of compounds on ion channels have been particularly challenging in the past, resulting in the limited exploitation of these targets.
The creation of cell-based assays tailored for use on different technologies represents a valuable tool for pharmaceutical companies. Axxam has created a comprehensive electrogenic
protein platform comprising several different ion channel and transporter cell-based assays, all of them optimized for HTS (384-MTP format) and uHTS (1536-MTP format).
Our extensive experience in cell-based assay generation allows us to select, case by case, the most suited reporter system for detecting functional activation of the channel. We consider not only the ion permeability of the transported ions but also the probability of obtaining good screening results to generate a reasonable hit rate.
Our proprietary Photina® technology is well suited for this purpose, being a very sensitive and reliable tool for detecting Ca2+ influx into the cells.
Additionally, all our assays are tested using the classic patch clamp technology - considered the gold standard reference technology.
We do this to validate results obtained with luminescence- or fluorescence-based methods on other instrumentation with a higher throughput but with lower information content compared to patch clamp. |
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