New Paper - DELs in micelles

High Fidelity Suzuki–Miyaura Coupling for the Synthesis of DNA Encoded Libraries Enabled by Micelle Forming Surfactants

Bioconjugate Chem. 2020, 31, 1, 149-155

https://doi.org/10.1021/acs.bioconjchem.9b00838         https://eprint.ncl.ac.uk/262771

James H. Hunter, Lisa Prendergast, Louis F. Valente, Andrew Madin, Garry Pairaudeau, Michael J. Waring*

Primarily the work of chemistry PhD student James Hunter and in collaboration with AstraZeneca, this work shows our method for synthesising DNA-encoded libraries using micellar technology.  We are applying these methods to building libraries that will be used in screening to more efficiently generate start points for our drug discovery programmes.

A highly efficient method of carrying out Suzuki-Miyaura couplings on DNA-conjugated substrates mediated by micellar surfactants was developed. The optimised protocol gives exceptionally clean (>98% on average) conversion to the desired birayl products across a diverse range of substrates and with no detectable DNA degradation.  This approach represents a step change from existing methods and will enable the production of DNA-encoded libraries with exceptionally high fidelity. 

Last modified: Mon, 19 Dec 2022 17:29:12 GMT