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A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase
Abstract
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or higher concentrations. PD 153035 rapidly suppressed autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocked EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD 153035 demonstrates an increase in potency over that of other tyrosine kinase inhibitors of four to five orders of magnitude for inhibition of isolated EGF receptor tyrosine kinase and three to four orders of magnitude for inhibition of cellular phosphorylation.
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“Four synthesized derivatives of 6- or 7-acrylamide-4-anilino-quinazolines, PD 160678 (70), PD 168393 (71), PD 160879 (72), PD 174265 (73), irreversibly inhibit EGFR TK activity with IC50 values 0.45–0.70 nM.”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [204]
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Metadata
- Authors
- Fry, D. W., Kraker, A. J., McMichael, A., Ambroso, L. A., Nelson, J. M., Leopold, W. R., Connors, R. W., & Bridges, A. J.
- Affiliations
- Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105.
- ORCID
- Nelson, James M.
- Venue
- Science
- Published
- 1994-08-19
- Volume
- 265
- Issue
- 5175
- Pages
- 1093-1095
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2069637592
- Cited by
- 806
- References
- 28
- Citations by year
- 2026: 8 · 2025: 8 · 2024: 10 · 2023: 9 · 2022: 10 · 2021: 12 · 2020: 19 · 2019: 11 · 2018: 13 · 2017: 18 · 2016: 13 · 2015: 18 · 2014: 24 · 2013: 26 · 2012: 31
- FWCI
- 14.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Keywords
- epidermal growth factor receptor, tyrosine kinase inhibitors, receptor autophosphorylation, mitogenesis, oncogenic transformation, early gene expression, small molecule inhibitors, kinase specificity
- MeSH terms
- Animals, Cell Transformation, Neoplastic, Epidermal Growth Factor, Humans, Kinetics, Mitosis, Phosphorylation, Platelet-Derived Growth Factor, Protein-Tyrosine Kinases, Quinazolines, Tumor Cells, Cultured, Tyrosine, Gene Expression, Fibroblast Growth Factor 2, 3T3 Cells, Mice, ErbB Receptors
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