Development of novel HDAC inhibitors to selectively co-inhibit HDAC8 and HDAC10 in childhood cancer
F Kolbinger, E Koeneke, J Senger, T Heimburg, T Bayer, M Jung, W Sippl, M Marek, C Romier, N Gunkel, AK Miller, P Sehr, O Witt, I Oehme · Klinische Pädiatrie · 2016 · Heft 05
Bibliografische Angaben
Zusammenfassung
Introduction: Histone deacetylases (HDACs) are validated targets in antitumoral therapy, and five pan-HDAC inhibitors have been clinically approved to date. Dosage of these inhibitors is limited due to side effects (e.g. leukopenia, diarrhea, fatigue) mainly attributed to HDAC1, 2 and 3 inhibition. High HDAC8 and high HDAC10 co-expression correlate with exceptionally poor outcomes in neuroblastoma. Preliminary studies employing siRNAs or sub-class selective HDAC inhibitors support our hypothesis that HDAC8/10 co-inhibition may yield therapeutic advantages. Results: To this end, ten novel small-molecule inhibitor…
