The DOI matches its Crossref record; 28 of the 28 references it cites were found in a registry or an index.
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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Oncogenes and signal transduction
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Growth factor signaling by receptor tyrosine kinases
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RECEPTORS FOR EPIDERMAL GROWTH FACTOR AND OTHER POLYPEPTIDE MITOGENS
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Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors
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- HENDLER, F. J., Increased EGF-R1 binding predicts a poor survival in squamous tumors, CANCER CELLS 7: 347 (1989).
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BindingDB Entry 50016732: The Ascension of Targeted Covalent Inhibitors.
BindingDB (2023) · UC San Diego · doi:10.7270/q23f4tpf
BindingDB Entry 50003985: Characterization of chemical libraries for luciferase inhibitory activity.
BindingDB (2020) · UC San Diego · doi:10.7270/q2f192hz
BindingDB Entry 50015722: Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.
BindingDB (2023) · UC San Diego · doi:10.7270/q2hq43wx
BindingDB (2026) · UC San Diego · doi:10.7270/q2rv0tkm
BindingDB Entry 4253: Synthesis and target identification of hymenialdisine analogs.
BindingDB (2011) · UC San Diego · doi:10.7270/q2fn14m9
BindingDB (2012) · UC San Diego · doi:10.7270/q23j3dhw
Kalthoff, H., Voss, M. M., Ungefroren, H., & Kremer, B. (1997) · Springer eBooks · doi:10.1007/978-3-642-60765-3_11
Rinehart (2000) · doi:10.1002/(sici)1098-1128(200001)20:1
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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