Axl Kinase as a Key Target for Oncology: Focus on Small Molecule Inhibitors

作者:Feneyrolles Clemence; Spenlinhauer Aurelia; Guiet Lea; Fauvel Benedicte; Dayde Cazals Benedicte; Warnault Pierre; Cheve Gwenael; Yasri Aziz*
来源:Molecular Cancer Therapeutics, 2014, 13(9): 2141-2148.
DOI:10.1158/1535-7163.MCT-13-1083

摘要

Receptor tyrosine kinases (RTK) are transmembrane receptors that regulate signal transduction in cells. As a member of the TAM (Tyro-3, Axl, Mer) RTK subfamily, Axl regulates key processes such as cell growth, migration, aggregation, and apoptosis through several pathways. Its overexpression/overactivation has been underlined in several conditions, especially cancers, and in both chemotherapy and targeted therapy sensitivity loss. In this review, we propose to highlight the therapeutic implication of Axl, starting with the pathways it regulates, validating its interest as a therapeutic target, and defining the tools available to develop strategies for its inhibition. We especially focus on small molecule inhibitors, their structure, inhibition profile, and development stages.

  • 出版日期2014-9