Axl kinase as a key target for oncology: focus on small molecule inhibitors.

نویسندگان

  • Clémence Feneyrolles
  • Aurélia Spenlinhauer
  • Léa Guiet
  • Bénédicte Fauvel
  • Bénédicte Daydé-Cazals
  • Pierre Warnault
  • Gwénaël Chevé
  • Aziz Yasri
چکیده

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.

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عنوان ژورنال:
  • Molecular cancer therapeutics

دوره 13 9  شماره 

صفحات  -

تاریخ انتشار 2014