Cited by 830HER2/EGFR in Cancer ResearchLung Cancer Treatments and MutationsProtein Kinase Regulation and GTPase Signaling

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A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase

Fry, David W., Kraker, Alan J., McMichael, Amy, Ambroso, Linda A., Nelson, James M., Leopold, Wilbur R., Connors, Richard W., Bridges, Alexander J.·1994·Science

DOI 10.1126/science.8066447

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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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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
Publisher: American Association for the Advancement of Science (AAAS)
Published: 1994-08-19
Volume: 265
Issue: 5175
Pages: 1093-1095
ISSN: 0036-8075 (ISSN-L)
1095-9203
DOI: 10.1126/science.8066447
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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A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase

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