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The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia

Tijdschriftbijdrage - Tijdschriftartikel

Human exportin-1 (XPO1) is the key nuclear-cytoplasmic transport protein that exports many cargo proteins out of the nucleus. Inducing nuclear accumulation of these proteins by inhibition of XPO1 causes cancer cell death. First clinical validation of pharmacological inhibition of XPO1 was obtained with the Selective Inhibitor of Nuclear Export (SINE) compound selinexor (KPT-330) demonstrating activity in Phase-II/IIb clinical trials when dosed 1 - 3 times weekly. The second-generation SINE compound KPT-8602 shows improved tolerability and can be dosed daily. Here we investigate and validate the drug-target interaction of KPT-8602 and explore its activity against acute lymphoblastic leukemia (ALL).
Tijdschrift: CLINICAL CANCER RESEARCH
ISSN: 1078-0432
Issue: 10
Volume: 23
Pagina's: 2528 - 2541
Jaar van publicatie:2017
BOF-keylabel:ja
IOF-keylabel:ja
BOF-publication weight:6
CSS-citation score:2
Auteurs:International
Authors from:Higher Education
Toegankelijkheid:Open