New high throughput screening and evolution method

CONECTUS ALSACE



28 Juillet 2015

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Fields

Biology / Medical

Sectors

Health
  • 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
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