State of the art
- DNA-encoded libraries (DELs) are emerging tools for the identification of biologically active compounds in pharmaceutical research. DEL technology is complementary to the classical screening approaches (e.g. HTS, fragments).
- Success of DELs highly depends on the diversity of such libraries. However, currently the number of chemical reactions for on DNA chemistry is limited. Reaction conditions must be compatible with the DNA itself, and therefore, the transformations are carried out in highly diluted, aqueous media.
Scheme 14. DNA-encoded libraries via photoredox chemistry.
Progress beyond the state of the art
- To the best of our knowledge, only 3 photochemical transformations have been applied to enable DEL synthesis so far.16
- We believe that photoredox catalysis is ideally suited to prepare DELs due to mild reaction conditions (room temperature catalysis, visible light, no strong oxidants or reductants) (Scheme 14).
- We will expand the number of transformations available in the area using the PhotoCube Pro instrument co-developed by CIX and ThalesNano.
- With the aid of the other partners, we will discover new photochemical transformations appropriate for DEL synthesis (at least two). Perform validation using DNA head-pieces.
- Prepare a mini-library for proof of concept (100-1000 members).