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Covalent Alkynylpyridopyrimidinones Targeting Cysteine 775 of the Epidermal Growth Factor Receptor Overcome Resistance to Current Therapies

Lookup NU author(s): Dr Hannah StewartORCiD, Dr Claire Jennings, Dr Islam Al-Khawaldeh, Dr Mathew MartinORCiD, Dr Richard NobleORCiD, Nicole Phillips, Sara Pintar, Dr Lisa PrendergastORCiD, Huw ThomasORCiD, Dr Jessica WattORCiD, Dr Anita Wittner, Dr Agnieszka Bronowska, Dr Celine CanoORCiD, Professor Martin NobleORCiD, Professor Steve WedgeORCiD, Professor Mike WaringORCiD

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This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).

Publication metadata

Author(s): Stewart HL, Bordoni C, Jennings CE, Al-Khawaldeh I, Martin MP, Noble RA, Phillips N, Pintar S, Prendergast L, Thomas HD, Wang L-Z, Watt JE, Wittner A, Bronowska AK, Cano C, Noble MEM, Wedge SR, Waring MJ

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2026

Volume: 69

Issue: 1

Pages: 533-552

Online publication date: 23/12/2025

Acceptance date: 12/12/2025

Date deposited: 20/01/2026

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804

Publisher: American Chemical Society

URL: https://doi.org/10.1021/acs.jmedchem.5c02924

DOI: 10.1021/acs.jmedchem.5c02924

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Funding

Funder referenceFunder name
Astex Pharmaceuticals (Newcastle Drug Discovery Alliance)
Cancer Research UK (Drug Discovery programme grants : C2115/A21421, DRCDDRPGMApr2020\100002)
the Medical Research Council (Developmental Pathways Funding Scheme, MR/X004872/1)

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