TY - JOUR
T1 - AXL inhibitors in cancer
T2 - A medicinal chemistry perspective
AU - Myers, Samuel H
AU - Brunton, Valerie G
AU - Unciti-Broceta, Asier
PY - 2015/11/10
Y1 - 2015/11/10
N2 - 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.
AB - 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.
U2 - 10.1021/acs.jmedchem.5b01273
DO - 10.1021/acs.jmedchem.5b01273
M3 - Article
C2 - 26555154
SN - 0022-2623
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
ER -