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| Title | Covalent Alkynylpyridopyrimidinones Targeting Cysteine 775 of the Epidermal Growth Factor Receptor Overcome Resistance to Current Therapies. |
|---|---|
| Journal, issue, pages | J. Med. Chem., Vol. 69, Page 533-552, Year 2026 |
| Publish date | Oct 17, 2024 (structure data deposition date) |
Authors | Stewart, H.L. / Bordoni, C. / Jennings, C.E. / Al-Khawaldeh, I. / Martin, M.P. / Noble, R.A. / Phillips, N. / Pintar, S. / Prendergast, L. / Thomas, H.D. ...Stewart, H.L. / Bordoni, C. / Jennings, C.E. / Al-Khawaldeh, I. / Martin, M.P. / Noble, R.A. / Phillips, N. / Pintar, S. / Prendergast, L. / Thomas, H.D. / Wang, L.Z. / Watt, J.E. / Wittner, A. / Bronowska, A.K. / Cano, C. / Noble, M.E.M. / Wedge, S.R. / Waring, M.J. |
External links | J. Med. Chem. / PubMed:41432179 |
| Methods | X-ray diffraction |
| Resolution | 2.423 - 3.163 Å |
| Structure data | ![]() PDB-9h42: ![]() PDB-9h46: ![]() PDB-9h47: ![]() PDB-9s3x: |
| Chemicals | ![]() PDB-1ir8: ![]() PDB-1isa: ![]() ChemComp-HOH: ![]() PDB-1ir9: ![]() PDB-1jlu: |
| Source |
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Keywords | TRANSFERASE / KINASE / EGFR / INHIBITOR / covalent |
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homo sapiens (human)
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