Targeting Focal Adhesion Kinase Using Inhibitors of Protein-Protein Interactions.
Fiche publication
Date publication
août 2018
Journal
Cancers
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DUJARDIN Denis, Dr RONDE Philippe
Tous les auteurs :
Mousson A, Sick E, Carl P, Dujardin D, De Mey J, Rondé P
Lien Pubmed
Résumé
Focal adhesion kinase (FAK) is a cytoplasmic non-receptor protein tyrosine kinase that is overexpressed and activated in many human cancers. FAK transmits signals to a wide range of targets through both kinase-dependant and independent mechanism thereby playing essential roles in cell survival, proliferation, migration and invasion. In the past years, small molecules that inhibit FAK kinase function have been developed and show reduced cancer progression and metastasis in several preclinical models. Clinical trials have been conducted and these molecules display limited adverse effect in patients. FAK contain multiple functional domains and thus exhibit both important scaffolding functions. In this review, we describe the major FAK interactions relevant in cancer signalling and discuss how such knowledge provide rational for the development of Protein-Protein Interactions (PPI) inhibitors.
Mots clés
FAK, FAK inhibitor, PPI inhibitor, cancer signalling
Référence
Cancers (Basel). 2018 Aug 21;10(9):