Fragment expansion with NUDELs – poised DNA-encoded libraries-Reference-Cited by-同舟云学术

Fragment expansion with NUDELs – poised DNA-encoded libraries

Published:2023 Issue:31 Volume:14 Page:8288-8294
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Salvini Catherine L. A.¹,Darlot Benoit²³,Davison Jack¹,Martin Mathew P.⁴,Tudhope Susan J.⁴,Turberville Shannon⁴,Kawamura Akane²³,Noble Martin E. M.⁴,Wedge Stephen R.⁴,Crawford James J.⁵^ORCID,Waring Michael J.¹^ORCID

Affiliation:

1. Cancer Research Horizons Therapeutic Innovation Newcastle Drug Discovery Group, Chemistry, School of Natural and Environmental Sciences, Newcastle University, Bedson Building, NE1 7RU, UK

2. Chemistry, School of Natural and Environmental Sciences, Newcastle University, Bedson Building, NE1 7RU, UK

3. Department of Chemistry, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK

4. Cancer Research Horizons Therapeutic Innovation Newcastle Drug Discovery Group, Translational and Clinical Research Institute, Newcastle University, Paul O'Gorman Building, NE2 4HH, UK

5. Genentech Inc., 1 DNA Way, South San Francisco, California, 94080, USA

Abstract

Fragment growing using poised DNA-encoded libraries, which allow the coupling of a targeted active fragment, allows the optimisation of fragment hits to potent compounds in a single operation, illustrated by the discovery of a 51 nM BRD4 ligand.

Funder

Genentech

Engineering and Physical Sciences Research Council

Cancer Research UK

Horizon 2020

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/SC/D3SC01171B

Reference29 articles.