Any Drug target, Any modality
1: Select your drug target
1: Select your drug target
1: Select your drug target
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.
2: Design reporter cells
1: Select your drug target
1: Select your drug target
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.
3: Test your drug candidates
4: Detect cell target engagement
4: Detect cell target engagement
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.
4: Detect cell target engagement
4: Detect cell target engagement
4: Detect cell target engagement
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.