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Lookup NU author(s): Dr Harriet Annabella Stanway-Gordon, Jake Odger, Professor Mike Waring
This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).
The capability of DNA encoded libraries (DELs) as a method of small molecule hit identification is becoming widely established in drug discovery. While their selection method offers advantages over more traditional means, DELs are limited by the chemistry that can be utilized to construct them. Significant advances in DNA compatible chemistry have been made over the past five years; however such procedures are still often burdened by substrate specificity and/or incomplete conversions, reducing the fidelity of the resulting libraries. One such reaction is the Heck coupling, for which current DNA-compatible protocols are somewhat unreliable. Utilizing micellar technology, we have developed a highly efficient DNA-compatible Heck reaction that proceeds on average to 95% conversion to product across a broad variety of structurally significant building blocks and multiple DNA conjugates. This work continues the application of micellar catalysis to the development of widely applicable, effective DNA-compatible reactions for use in DELs.
Author(s): Stanway-Gordon HA, Odger JA, Waring MJ
Publication type: Article
Publication status: Published
Journal: Bioconjugate Chemistry
Year: 2023
Volume: 34
Issue: 4
Pages: 756-763
Print publication date: 19/04/2023
Online publication date: 08/03/2023
Acceptance date: 08/03/2023
Date deposited: 21/03/2023
ISSN (print): 1043-1802
ISSN (electronic): 1520-4812
Publisher: American Chemical Society
URL: https://doi.org/10.1021/acs.bioconjchem.3c00051
DOI: 10.1021/acs.bioconjchem.3c00051
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