title: AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.
abstract: 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.
authors.affiliation: Edinburgh Cancer Research UK Centre, MRC Institute of Genetics and Molecular Medicine, University of Edinburgh , Crewe Road South, Edinburgh EH4 2XR, U.K.
authors.forename: Samuel H
authors.initials: SH
authors.lastname: Myers
authors.affiliation: Edinburgh Cancer Research UK Centre, MRC Institute of Genetics and Molecular Medicine, University of Edinburgh , Crewe Road South, Edinburgh EH4 2XR, U.K.
authors.forename: Valerie G
authors.initials: VG
authors.lastname: Brunton
authors.affiliation: Edinburgh Cancer Research UK Centre, MRC Institute of Genetics and Molecular Medicine, University of Edinburgh , Crewe Road South, Edinburgh EH4 2XR, U.K.
authors.forename: Asier
authors.initials: A
authors.lastname: Unciti-Broceta
mesh_terms: D002626:Chemistry, Pharmaceutical; D006801:Humans; D009369:Neoplasms / Q000201:enzymology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D000094963:Axl Receptor Tyrosine Kinase
chemical_list: D047428:Protein Kinase Inhibitors; D011518:Proto-Oncogene Proteins; D020794:Receptor Protein-Tyrosine Kinases; D000094963:Axl Receptor Tyrosine Kinase; C000722289:AXL protein, human