ArticleProceedings of the National Academy of Sciences of the United States of America1994
4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
17 citing papers in PubMed, 99 citations in OpenAlex.
- Vinyl azides in organic synthesis: an overview.RSC advances · 2023Review
- α1-Adrenoceptor-mediated contraction of rat aorta is partly mediated via transactivation of the epidermal growth factor receptor.British journal of pharmacology · 2010Article
- Article
- Erk5 participates in neuregulin signal transduction and is constitutively active in breast cancer cells overexpressing ErbB2.Molecular and cellular biology · 2002Article
- Review
- Specific inhibitors of platelet-derived growth factor or epidermal growth factor receptor tyrosine kinase reduce pulmonary fibrosis in rats.The American journal of pathology · 1999Article
- The transcription factor AP-1 is required for EGF-induced activation of rho-like GTPases, cytoskeletal rearrangements, motility, and in vitro invasion of A431 cells.The Journal of cell biology · 1998Article
- The Croonian Lecture 1997. The phosphorylation of proteins on tyrosine: its role in cell growth and disease.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 1998Review
- Epidermal growth factor receptor and the adaptor protein p52Shc are specific substrates of T-cell protein tyrosine phosphatase.Molecular and cellular biology · 1998Article
- Signal transduction pathways and their relevance in human astrocytomas.Journal of neuro-oncology · 1997Review
- Targeting signal transduction for disease therapy.Medical oncology (Northwood, London, England) · 1997Review
- Specific inhibition of epidermal growth factor receptor tyrosine kinase by 4-anilinoquinazolines.Breast cancer research and treatment · 1996Review
- Inhibition of signaling from Type 1 receptor tyrosine kinases via intracellular expression of single-chain antibodies.Breast cancer research and treatment · 1996Review
- Modelling study of protein kinase inhibitors: binding mode of staurosporine and origin of the selectivity of CGP 52411.Journal of computer-aided molecular design · 1995Article
- Neu differentiation factor activation of ErbB-3 and ErbB-4 is cell specific and displays a differential requirement for ErbB-2.Molecular and cellular biology · 1995Article
- Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class.Proceedings of the National Academy of Sciences of the United States of America · 1995Article
- Single-chain antibody-mediated intracellular retention of ErbB-2 impairs Neu differentiation factor and epidermal growth factor signaling.Molecular and cellular biology · 1995Article
Corrections and comments
- Retraction · 1998-09-29Error in Analyses · Error in Results and/or Conclusions ·
- RetractedRetractions.1998
Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Deregulated signal transduction via the epidermal growth factor receptor (EGF-R) family of protein-tyrosine kinase growth factor receptors is associated with proliferative diseases. We describe a class of compounds (4,5-dianilinophthalimides) that inhibit the EGF-R protein-tyrosine kinase in vitro with high selectivity. In cells, 4,5-dianilinophthalmide selectively inhibited both ligand-induced EGF-R and p185c-erbB2 autophosphorylation and c-fos mRNA induction. Antitumor activity could be demonstrated in vivo against xenografts of the A431 and SK-OV-3 tumors, which overexpress the EGF-R and p185c-erbB2, respectively. In contrast, a platelet-derived growth factor-driven tumor was not inhibited by 4,5-dianilinophthalimide, which is compatible with its cellular selectivity and hypothesized mechanism of action. No overt cumulative toxicity was observed during treatment even though high efficacy was observed, indicating a good therapeutic window. 4,5-Dianilinophthalimides may offer therapeutic agents for the treatment of hyperproliferative diseases that overexpress EGF-R family protein-tyrosine kinases or their ligands.
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