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Updated: Aug 17, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Tyrosine kinase src inhibitors: potential therapeutic applications
1Department of Arthritis and Bone Metabolism, Unit Bone Metabolism, Research Bone Metabolism, Novartis Pharma AG, Basel, Switzerland.
Abstract:
More than 20 years after its discovery, tyrosine kinase Src is still the focus of intense research, in both academia and the pharmaceutical industry. A prototype for non-receptor tyrosine kinases and proto-oncogenes, Src also has a specific role in bone biology. Src's essential role in osteoclast-mediated bone resorption relies on its high expression in this cell type and on the presence of specific substrates, the identity of which is currently being unraveled. Recent identification of selective, potent and orally available Src family kinase inhibitors and their detailed characterization in cells and in animal models of bone loss has produced a new impetus and a novel tool in the field. Here we review the cellular and molecular mechanisms through which Src kinase inhibitors could find an application as therapeutics, particularly in the fields of bone and cancer-induced bone metastases.
Insights
Tyrosine kinase Src plays a key role in bone resorption. New Src family kinase inhibitors show therapeutic potential for bone loss and bone metastases, offering a novel treatment strategy.
Area of Science:
- Biochemistry
- Oncology
- Bone Biology
Background:
- The tyrosine kinase Src is a proto-oncogene and a prototype for non-receptor tyrosine kinases.
- Src has a critical role in osteoclast function and bone resorption.
- Research into Src's specific substrates and functions is ongoing.
Purpose of the Study:
- To review the cellular and molecular mechanisms of Src kinase inhibitors.
- To explore the therapeutic potential of Src kinase inhibitors in bone diseases and cancer-induced bone metastases.
Main Methods:
- Review of recent scientific literature on Src kinase inhibitors.
- Analysis of cellular and animal models of bone loss.
- Characterization of selective, potent, and orally available Src family kinase inhibitors.
Main Results:
- Src family kinase inhibitors have been identified and characterized.
- These inhibitors demonstrate potential in preclinical models of bone loss.
- The mechanisms through which these inhibitors act are being elucidated.
Conclusions:
- Src kinase inhibitors represent a novel therapeutic tool.
- They hold promise for treating bone disorders and bone metastases from cancer.
- Further research into their application is warranted.
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