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AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective

Samuel H Myers1, Valerie G Brunton1, Asier Unciti-Broceta1

  • 1Edinburgh Cancer Research UK Centre, MRC Institute of Genetics and Molecular Medicine, University of Edinburgh , Crewe Road South, Edinburgh EH4 2XR, U.K.

Journal of Medicinal Chemistry
|November 12, 2015
PubMed

Insights

Targeting the AXL receptor tyrosine kinase is crucial for cancer treatment due to its link to poor prognosis and drug resistance. This review discusses AXL inhibitors and their therapeutic potential.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Dysregulation of the AXL receptor tyrosine kinase is implicated in various cancers.
  • AXL signaling is increasingly recognized for its association with poor patient prognosis and resistance to cancer therapies.
  • The development of AXL inhibitors represents a significant advancement in cancer treatment strategies.

Purpose of the Study:

  • To review the chemical and biological properties of key AXL inhibitors.
  • To evaluate the current clinical contribution and future potential of AXL inhibition in cancer therapy.
  • To identify the prospects and challenges in translating AXL inhibitors into effective therapeutic options.

Main Methods:

  • Literature review of AXL inhibitors in clinical trials and development.
  • Analysis of chemical structures and biological activities of targeted and off-target AXL inhibitors.
  • Evaluation of clinical data and preclinical studies related to AXL inhibition.

Main Results:

  • Several kinase inhibitors, both approved and in development, target AXL, either primarily or secondarily.
  • The first AXL-specific inhibitor entered clinical trials in 2013, marking a milestone in AXL-targeted therapy.
  • Accumulating evidence highlights AXL's role in cancer progression and therapeutic resistance.

Conclusions:

  • AXL inhibition holds significant promise as a therapeutic strategy in oncology.
  • Understanding the properties of various AXL inhibitors is crucial for optimizing their clinical application.
  • Overcoming challenges in AXL inhibitor development is essential for their successful translation into bona fide cancer treatments.

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