title: Axl kinase as a key target for oncology: focus on small molecule inhibitors.
abstract: 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.
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Clémence
authors.initials: C
authors.lastname: Feneyrolles
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Aurélia
authors.initials: A
authors.lastname: Spenlinhauer
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Léa
authors.initials: L
authors.lastname: Guiet
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Bénédicte
authors.initials: B
authors.lastname: Fauvel
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Bénédicte
authors.initials: B
authors.lastname: Daydé-Cazals
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Pierre
authors.initials: P
authors.lastname: Warnault
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France.
authors.forename: Gwénaël
authors.initials: G
authors.lastname: Chevé
authors.affiliation: OriBase Pharma, Cap Gamma, Montpellier, France ayasri@oribase-pharma.com.
authors.forename: Aziz
authors.initials: A
authors.lastname: Yasri
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D008495:Medical Oncology / Q000379:methods*; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000628:therapy*; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D015398:Signal Transduction; D000094963:Axl Receptor Tyrosine Kinase
chemical_list: D000970:Antineoplastic Agents; D011518:Proto-Oncogene Proteins; D020794:Receptor Protein-Tyrosine Kinases; D000094963:Axl Receptor Tyrosine Kinase; C000722289:AXL protein, human