Small molecule inhibitors of the transmembrane receptor tyrosine kinase Axl as potential anti-cancer therapeutics


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Azadeh Bagherzadeh1, Neil Jones1, Michelle Barnard1, Alexandra Boakes1, Timo Heikkila1, James Firth1, Gregoire Pave1, Emma Wynne1, Francesca Blum1, Irene Farr Gutierrez1, Kevin Stewart1, Aurore Lejeune1, Tim Hammonds1, Alan Storey3, Edel OToole2, Lorna Stewart1, Laurent Rigoreau1

1Cancer Research Technology Discovery Lab, London, UK, 2Barts and London School of Medicine and Dentistry, Queen Mary, University of London, UK, 3Weatherall Institute of Molecular Medicine, University of Oxford, John Radcliffe Hospital, UK

Abstract

Following stimulation by its endogenous ligand Gas6, the transmembrane receptor tyrosine kinase (RTK) Axl mediates oncogenic transformation through its intracellular kinase domain (ICD).