Validating engagement of drug candidates with therapeutic targets is a challenge in drug discovery. The MICRO-TAG technology is the 3rd generation of cellular target engagement technology. It enables interrogation of target engagement without interfering with folding, localization, and function of target proteins, all within the physiological milieu of the cell.
Choose your target: from literature review, proteomics analysis, synthetic lethality screen etc. You may choose to work with multiple versions of the same target, such as its isoforms or mutants. Human or non-human targets. Consider undruggable targets as well.
Every drug target has a unique fingerprint. Responsive cell systems are designed for every target. For an initial pilot test, transient expression can be sufficient. Stable reporter cells may be engineered using lentiviral or CRISPR methods.
Reporter cells designed for your drug target can be tested with your ligands. The cells will be challenged at Temperature of aggregation (T-agg), a temperature point at which your target is in a structurally fluid state. This responsive system will enable fast hit to lead discovery.
Signal is detected by addition of Micro-Tag-binding protein and FRET substrate by virtue of enzyme complementation. The level of signal is directly proportional to the level of stabilized target. Potency of cell target engagement can be calculated. This system is sensitive to conventional and undruggable targets.
Use the native context of the cell to test drug targets. Preserve the therapeutic function of the target by choosing the relevant cell type.
Tap into the opportunity of challenging drug targets such as transcription factors, membrane proteins etc.
Work with highly responsive cell systems designed for your drug target of interest. Identify drug candidates that engage the target in the cell.
Empower your drug discovery program with real-time cell target engagement data. Reveal in-cell kinetics of drug-target engagement.
Augment your drug discovery with the power of Artificial Intelligence. Screen bigger libraries and work with novel drug targets.
Scale your drug discovery effort for success. Use our sensitive cell systems for discovery and validation of novel drug candidates.
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