New high throughput screening and evolution method

• Fragment-based drug discovery approach using PNA-tagged ligands
• Technology accelerating identification of leads or validation of novel therapeutic target
• Fast evolution process to select high affinity ligands
• Cost effective

TECHNOLOGY

Iterative screening strategy based on PNA-encoded libraries

1- Combinatorial assembly of PNA-tagged molecule libraries by hybridisation to a complementary DNA-template library

2- Selection of the DNA-templated combinatorial library against an immobilised target

3- Amplification of the selected library

4- Reiteration of the cycle of selection/ amplification

APPLICATIONS

• Fragment-based drug discovery
• Hit generation and hit to lead optimisation
• Generation of tools for the validation of new therapeutic targets

INNOVATION ADVANTAGES

• Fragment-based HTS
• Libraries of unprecedented size and broader diversity
• Fast screening (2 cycles of selection/amplification per day)
• Miniaturised technology requiring low amounts of target protein and libraries
• Can detect weak affinity fragments
• PNA libraries allow for more permissive chemistry, high affinity and stability
• Low investment needed to be set-up