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Updated: Jun 10, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Receptor tyrosine kinases as therapeutic targets in cancer
1Friedrich Miescher Institute for Biomedical Research, Maulbeerstrasse 66, CH-4059 Basel, Switzerland.
Abstract:
Extract: Tyrosine kinases are a large and diverse family of proteins found only in Metazoans. The ERBB receptor tyrosine kinases (RTK), the main focus of this article, belong to the sub-group encompassing the cell surface proteins. All receptor tyrosine kinases have an extracellular domain that binds peptide ligands, span the membrane once, and have an intracellular portion with protein tyrosine kinase activity. Ligand binding to receptor tyrosine kinases induces the formation of receptor dimers and activates the kinase domain of the receptor, which transfers a phosphate group from the bound ATP to specific tyrosine side chains on the receptor proteins and on intracellular signaling proteins that bind the active receptor tyrosine kinases. In many types of human tumors, ERBB (erythroblastosis group B) receptor tyrosine kinases are aberrantly activated and contribute to cancer development. Accordingly, these receptors have been intensely studied both to understand their roles in cancer biology and to employ them as therapeutic targets. Many ERBB targeted inhibitors are now in clinical use.
Insights
Erythroblastosis group B (ERBB) receptor tyrosine kinases are key proteins in cell signaling. Aberrant activation of these ERBB receptors drives human tumor development, making them important therapeutic targets.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Receptor tyrosine kinases (RTKs) are cell surface proteins crucial for signal transduction.
- ERBB receptors, a subgroup of RTKs, possess extracellular ligand-binding domains and intracellular kinase activity.
- These receptors activate intracellular signaling pathways upon ligand binding and dimerization.
Purpose of the Study:
- To review the role of ERBB receptor tyrosine kinases in human cancer.
- To highlight ERBB receptors as significant therapeutic targets in oncology.
- To discuss the development of ERBB-targeted inhibitors.
Main Methods:
- Literature review focusing on ERBB receptor tyrosine kinases.
- Analysis of the structure and function of ERBB receptors.
- Examination of the aberrant activation of ERBB in human tumors.
- Overview of current therapeutic strategies targeting ERBB.
Main Results:
- ERBB receptor tyrosine kinases are frequently hyperactivated in various human cancers.
- This aberrant activation contributes significantly to tumorigenesis and cancer progression.
- Targeted inhibitors against ERBB receptors have shown clinical efficacy.
Conclusions:
- ERBB receptor tyrosine kinases play a critical role in cancer biology.
- Understanding ERBB signaling is vital for developing effective cancer therapies.
- Targeted inhibition of ERBB receptors represents a successful therapeutic strategy in oncology.
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