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Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors
Abstract
A systematic series of low molecular weight protein tyrosine kinase inhibitors were synthesized; they had progressively increasing affinity over a 2500-fold range toward the substrate site of epidermal growth factor (EGF) receptor kinase domain. These compounds inhibited EGF receptor kinase activity up to three orders of magnitude more than they inhibited insulin receptor kinase, and they also effectively inhibited the EGF-dependent autophosphorylation of the receptor. The most potent compounds effectively inhibited the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on the EGF-independent proliferation of these cells. The potential use of tyrosine protein kinase inhibitors as antiproliferative agents is demonstrated.
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Citations
Cited by
Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells
Druker, B. J., Tamura, S., Buchdunger, E., Ohno, S., Segal, G. M., Fanning, S., Zimmermann, J., & Lydon, N. B. (1996) · Nature Medicine · doi:10.1038/nm0596-561 · Cited by 2,967
The discovery of receptor tyrosine kinases: targets for cancer therapy
Gschwind, A., Fischer, O. M., & Ullrich, A. (2004) · Nature Reviews Cancer · doi:10.1038/nrc1360 · Cited by 1,227
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Druker, B. J. (2008) · Blood · doi:10.1182/blood-2008-07-077958 · Cited by 668
Tyrosine kinase – Role and significance in Cancer
Paul, M. K., & Mukhopadhyay, A. K. (2004) · International Journal of Medical Sciences · doi:10.7150/ijms.1.101 · Cited by 624
Clinical pharmacokinetics of tyrosine kinase inhibitors
van Erp, N. P., Gelderblom, H., & Guchelaar, H.-J. (2009) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2009.08.004 · Cited by 503
Metadata
- Authors
- Yaish, P., Gazit, A., Gilon, C., & Levitzki, A.
- Venue
- Science
- Published
- 1988-11-11
- Volume
- 242
- Issue
- 4880
- Pages
- 933-935
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2020707154
- Cited by
- 587
- References
- 0
- FWCI
- 15.71
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors. https://app.cochat.ai/papers/10.1126/science.3263702
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- Yaish, P., Gazit, A., Gilon, C., & Levitzki, A. (1988). Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors. Science. https://doi.org/10.1126/science.3263702
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
