Conditional inhibitors allow modulation of a target’s function by identifying a unique context or “condition” of the target that is functionally relevant for tumor development and growth.
The conditional inhibitor only modulates the target when it is in that condition, and NOT under other conditions.
Such conditions might involve:
- Post-translational modifications that regulate the target protein’s oncogenic function.
- Distinct functional protein complexes that specifically lead to the target’s oncogenic function.
- The target protein’s location in the cell.
Advantages of Conditional Inhibition:
Inhibiting important targets under these functionally relevant conditions allows Cedilla to:
- Modulate the pathogenic function of the target, rather than the physiologic function.
- Decrease off-target toxicity, even where selectivity has been a historical challenge.
- Develop profiles suitable for combination therapy, in disease states where multiple targets are required to achieve and sustain anti-tumor effect.
After defining the parameters for a functionally relevant condition, Cedilla designs bespoke biophysical, biochemical, and cellular screens to mimic that specific condition as closely as possible.
This approach reveals novel binding sites and mechanisms of action, which in turn allows us to identify small molecules that inhibit or otherwise modulate the target in this disease-relevant context.
Learn more about our conditional inhibitors »