Recent discovery and development of AXL inhibitors as antitumor agents.
Eur J Med Chem
; 272: 116475, 2024 Jun 05.
Article
in En
| MEDLINE
| ID: mdl-38714043
ABSTRACT
AXL, a receptor tyrosine kinase (RTK), plays a pivotal role in various cellular functions. It is primarily involved in processes such as epithelial-mesenchymal transition (EMT) in tumor cells, angiogenesis, apoptosis, immune regulation, and chemotherapy resistance mechanisms. Therefore, targeting AXL is a promising therapeutic approach for the treatment of cancer. AXL inhibitors that have entered clinical trials, such as BGB324(1), have shown promising efficacy in the treatment of melanoma and non-small cell lung cancer. Additionally, novel AXL-targeted drugs, such as AXL degraders, offer a potential solution to overcome the limitations of traditional small-molecule AXL inhibitors targeting single pathways. We provide an overview of the structure and biological functions of AXL, discusses its correlation with various cancers, and critically analyzes the structure-activity relationship of AXL small-molecule inhibitors in cellular contexts. Additionally, we summarize multiple research and development strategies, offering insights for the future development of innovative AXL inhibitors.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Proto-Oncogene Proteins
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Receptor Protein-Tyrosine Kinases
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Protein Kinase Inhibitors
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Drug Discovery
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Axl Receptor Tyrosine Kinase
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Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Eur J Med Chem
/
Eur. j. med. chem
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European journal of medicinal chemistry
Year:
2024
Document type:
Article
Country of publication:
Francia