AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective

Dysregulation of the AXL receptor tyrosine kinase has been associated with many types of cancer. It has not been until recently, however, that targeting AXL has come under the spotlight because of ever accumulating evidence of its strong correlation with poor prognosis and drug resistance. The entry...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2016-04, Vol.59 (8), p.3593-3608
Main Authors: Myers, Samuel H, Brunton, Valerie G, Unciti-Broceta, Asier
Format: Article
Language:English
Subjects:
Chemistry, Pharmaceutical
Humans
Neoplasms - enzymology
Protein Kinase Inhibitors - pharmacology
Proto-Oncogene Proteins - antagonists & inhibitors
Receptor Protein-Tyrosine Kinases - antagonists & inhibitors
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Summary:Dysregulation of the AXL receptor tyrosine kinase has been associated with many types of cancer. It has not been until recently, however, that targeting AXL has come under the spotlight because of ever accumulating evidence of its strong correlation with poor prognosis and drug resistance. The entry of the first AXL-branded inhibitor in clinical trials in 2013 marked an important milestone for the clinical validation of AXL as an anticancer target. Nevertheless, to weigh the current contribution and potential future impact of AXL inhibition in the clinic, it is fundamental to recognize that several kinase inhibitors approved or in clinical development have AXL as either a prominent secondary or even the primary target. Through this review, the chemical and biological properties of the main inhibitors targeting AXL (either intentionally or unintentionally) will be discussed, along with the prospects and challenges to translate AXL inhibitors into a bona fide therapeutic option.
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.5b01273