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Recent discovery and development of AXL inhibitors as antitumor agents

Zihang Liu1, Li Chen2, Jifa Zhang3

  • 1Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-Related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, State Key Laboratory of Respiratory Health and Multimorbidity, Laboratory of Neuro-system and Multimorbidity, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, Sichuan, China.

European Journal of Medicinal Chemistry
|May 7, 2024
PubMed

Insights

Targeting AXL, a receptor tyrosine kinase, shows promise for cancer therapy. Novel AXL inhibitors and degraders offer new strategies to overcome resistance and improve treatment efficacy in various cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • AXL receptor tyrosine kinase (RTK) is implicated in key cellular processes including epithelial-mesenchymal transition (EMT), angiogenesis, apoptosis, immune regulation, and chemotherapy resistance.
  • Dysregulation of AXL signaling is associated with the progression and treatment resistance of various cancers.

Purpose of the Study:

  • To provide a comprehensive overview of AXL's structure and biological functions.
  • To analyze the correlation between AXL and diverse cancer types.
  • To critically evaluate the structure-activity relationships of small-molecule AXL inhibitors.

Main Methods:

  • Literature review and analysis of existing research on AXL.
  • Examination of clinical trial data for AXL inhibitors.
  • Structure-activity relationship (SAR) analysis of AXL inhibitors in cellular models.

Main Results:

  • AXL inhibitors, including BGB324, demonstrate efficacy in melanoma and non-small cell lung cancer.
  • AXL degraders represent a novel therapeutic strategy to overcome limitations of traditional inhibitors.
  • Understanding SAR is crucial for developing potent and selective AXL inhibitors.

Conclusions:

  • Targeting AXL is a viable therapeutic strategy for cancer treatment.
  • AXL degraders offer a promising avenue for overcoming resistance mechanisms.
  • Future research should focus on developing innovative AXL inhibitors based on SAR and diverse development strategies.
Keywords:
AXLCancerDrug discoveryInhibitorsStructure-activity relationship

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