Relocalization of KIT D816V to cell surface after dasatinib treatment: potential clinical implications.
Bougherara H, Georgin-Lavialle S, Damaj G, Launay JM, Lhermitte L, Auclair C, Arock M, Dubreuil P, Hermine O, Poul MA
Systemic mastocytosis (SM) is a heterogeneous disease that displays variable aggressivity. Adults with SM frequently have a D816V mutation in the tyrosine kinase (TK) receptor gene KIT. We previously reported that, in a Chinese hamster ovarian cell model expressing exogenous KIT variants, constitutive activating KIT mutations induced intracellular mislocalization of KIT reversed by inhibition of KIT TK activity. Hence, we hypothesized that inhibition of KIT kinase activity by the TK inhibitor dasatinib could be useful to increase KIT detection sensitivity in samples from patients with SM.Lire l‘article