AXL kinase inhibitors- A prospective model for medicinal chemistry strategies in anticancer drug discovery.

Chinmay Malvankar, Dileep Kumar

Biochimica et biophysica acta. Reviews on cancer 2022 Sep

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Deviant expressions of the tyrosine kinase AXL receptor are strongly correlated with a plethora of malignancies. Henceforth, the topic of targeting AXL is beginning to gain prominence due to mounting evidence of the protein's substantial connection to poor prognosis and treatment resistance. This year marked a milestone in clinical testing for AXL as an anti-carcinogenic target, with the start of the first AXL-branded inhibitor study. It is critical to emphasize that AXL is a primary and secondary target in various kinase inhibitors that have been approved or are on the verge of being approved while interpreting the present benefits and future potential effects of AXL suppression in the clinical setting. Several research arenas across the globe resolutely affirm the crucial significance of AXL receptors in the case study of several pathophysiologies including AML, prostate cancer, and breast cancer. This review endeavors to delve deeply into the biological, chemical, and structural features of AXL kinase; primary AXL inhibitors that target the enzyme (either purposefully or unintentionally); and the prospects and barriers for turning AXL inhibitors into a feasible treatment alternative. Furthermore, we analyse the co-crystal structure of AXL, which remains extensively unexplored, as well as the mutations of AXL that may be valuable in the development of novel inhibitors in the upcoming future and take a comprehensive look at the medicinal chemistry of AXL inhibitors of recent years. Copyright © 2022. Published by Elsevier B.V.

Citation

Chinmay Malvankar, Dileep Kumar. AXL kinase inhibitors- A prospective model for medicinal chemistry strategies in anticancer drug discovery. Biochimica et biophysica acta. Reviews on cancer. 2022 Sep;1877(5):188786