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Updated: Apr 25, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Axl kinase as a key target for oncology: focus on small molecule inhibitors
Clémence Feneyrolles1, Aurélia Spenlinhauer1, Léa Guiet1
1OriBase Pharma, Cap Gamma, Montpellier, France.
Abstract:
Receptor tyrosine kinases (RTK) are transmembrane receptors that regulate signal transduction in cells. As a member of the TAM (Tyro-3, Axl, Mer) RTK subfamily, Axl regulates key processes such as cell growth, migration, aggregation, and apoptosis through several pathways. Its overexpression/overactivation has been underlined in several conditions, especially cancers, and in both chemotherapy and targeted therapy sensitivity loss. In this review, we propose to highlight the therapeutic implication of Axl, starting with the pathways it regulates, validating its interest as a therapeutic target, and defining the tools available to develop strategies for its inhibition. We especially focus on small molecule inhibitors, their structure, inhibition profile, and development stages.
Insights
Axl receptor tyrosine kinase (RTK) is implicated in cancer progression and therapy resistance. This review explores Axl
Area of Science:
- Molecular Biology
- Cell Signaling
- Oncology
Background:
- Receptor tyrosine kinases (RTKs) are crucial transmembrane proteins regulating cellular signal transduction.
- The TAM (Tyro-3, Axl, Mer) subfamily RTKs, particularly Axl, play significant roles in cell growth, migration, aggregation, and apoptosis.
- Axl overexpression/overactivation is linked to various cancers and contributes to resistance against chemotherapy and targeted therapies.
Purpose of the Study:
- To highlight the therapeutic implications of Axl as a target in cancer treatment.
- To review the signaling pathways regulated by Axl.
- To define available tools and strategies for Axl inhibition.
Main Methods:
- Literature review focusing on Axl signaling pathways.
- Analysis of Axl's role in cancer and therapy resistance.
- Examination of small molecule inhibitors targeting Axl.
Main Results:
- Axl regulates critical cellular processes and its dysregulation is associated with oncogenesis.
- Axl inhibition presents a promising therapeutic strategy for overcoming treatment resistance.
- Various small molecule inhibitors targeting Axl have been developed with diverse structures and inhibition profiles.
Conclusions:
- Axl is a validated therapeutic target in oncology due to its role in cancer progression and drug resistance.
- Small molecule inhibitors targeting Axl are under active development, offering potential new treatment avenues.
- Further research into Axl inhibition strategies is warranted to improve cancer therapy outcomes.
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