AXL
A receptor that helps cancer cells survive stress, resist treatment and spread. Cabozantinib is among the multi-kinase drugs that block it, and dedicated AXL inhibitors and antibody-drug conjugates are in trials.
Overview
AXL, a TAM-family receptor activated by the ligand GAS6, drives epithelial-to-mesenchymal transition, invasion and immune suppression and is switched on as cancers become resistant to EGFR, ALK and BRAF inhibitors and to chemotherapy. Cabozantinib inhibits AXL alongside MET and VEGFR2, which is thought to contribute to its activity in kidney, liver and thyroid cancers after other treatments. Selective AXL inhibitors such as bemcentinib and the AXL-directed antibody-drug conjugate enapotamab vedotin have been tested without a clear win so far, and AXL remains a resistance target of high interest.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · A receptor that helps cancer cells survive stress, resist treatment and spread. Cabozantinib is among the multi-kinase drugs that block it, and dedicated AXL inhibitors and antibody-drug conjugates are in trials.
- 1 · What it is
A receptor that helps cancer cells survive stress, resist treatment and spread. Cabozantinib is among the multi-kinase drugs that block it, and dedicated AXL inhibitors and antibody-drug conjugates are in trials.
- 2 · What goes wrong in cancer
TAM-family receptor tyrosine kinase activated by GAS6; mediates mesenchymal transition and acquired resistance to targeted therapy.
- 3 · How drugs use it
No product in this corpus aims at AXL yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Biology
TAM-family receptor tyrosine kinase activated by GAS6; mediates mesenchymal transition and acquired resistance to targeted therapy.
- Kidney, liver and thyroid cancers treated with cabozantinib
- Drug-resistant lung cancer, melanoma and triple-negative breast cancer
Latest papers
topQuery for this target: (TITLE:"AXL" OR ABSTRACT:"AXL") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about AXL, not a curated reading list.
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