Targeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma
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- 作者：Jonas Ecker (1)
Ina Oehme (1)
Ralph Mazitschek (2) (3)
Andrey Korshunov (4) (5)
Marcel Kool (6) (7)
Thomas Hielscher (8)
Judit Kiss (1) (9)
Florian Selt (1) (9)
Carina Konrad (1)
Marco Lodrini (1) (10)
Hedwig E Deubzer (1) (10) (9)
Andreas von Deimling (4) (5)
Andreas E Kulozik (9)
Stefan M Pfister (6) (7) (9)
Olaf Witt (1) (9)
Till Milde (1) (9)
1. Clinical Cooperation Unit Pediatric Oncology (G340) ; German Cancer Research Center (DKFZ) ; Im Neuenheimer Feld 280 ; 69120 ; Heidelberg ; Germany
2. Center for Systems Biology ; Massachusetts General Hospital ; Boston ; MA ; 02114 ; USA
3. The Broad Institute of Harvard and MIT ; Cambridge ; Massachusetts ; 02142 ; USA
4. Department of Neuropathology ; University Hospital Heidelberg ; Im Neuenheimer Feld 224 ; 69120 ; Heidelberg ; Germany
5. Clinical Cooperation Unit Neuropathology (G380) ; German Cancer Research Center (DKFZ) ; and German Cancer Consortium (DKTK) ; Heidelberg ; Germany
6. Division of Pediatric Neurooncology (B062) ; German Cancer Research Center (DKFZ) ; Heidelberg ; Germany ; and German Cancer Consortium (DKTK) ; Heidelberg ; Germany
7. German Cancer Consortium (DKTK) ; Heidelberg ; Germany
8. Division of Biostatistics (C060) ; German Cancer Research Center (DKFZ) ; Heidelberg ; Germany
9. Section of Pediatric Brain Tumors ; Department of Pediatric Oncology ; Hematology and Immunology ; University Hospital Heidelberg ; Im Neuenheimer Feld 430 ; 69120 ; Heidelberg ; Germany
10. Department of Pediatric Hematology ; Oncology and Bone Marrow Transplantation ; Charit茅 - University Medicine Berlin ; CVK ; CC17 ; Augustenburger Platz 1 ; 13353 ; Berlin ; Germany - 关键词：Medulloblastoma ; HDAC ; HDAC inhibitor ; HDAC2 ; MYC
- 刊名：Acta Neuropathologica Communications
- 出版年：2015
- 出版时间：December 2015
- 年：2015
- 卷：3
- 期：1
- 全文大小：1,426 KB
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- 出版者：BioMed Central
- ISSN：2051-5960
文摘
Introduction Medulloblastoma (MB) is the most frequent malignant brain tumor in children. Four subgroups with distinct genetic, epigenetic and clinical characteristics have been identified. Survival remains particularly poor in patients with Group 3 tumors harbouring a MYC amplification. We herein explore the molecular mechanisms and translational implications of class I histone deacetylase (HDAC) inhibition in MYC driven MBs. Material and Methods Expression of HDACs in primary MB subgroups was compared to normal brain tissue. A panel of MB cell lines, including Group 3 MYC amplified cell lines, were used as model systems. Cells were treated with HDAC inhibitors (HDACi) selectively targeting class I or IIa HDACs. Depletion of HDAC2 was performed. Intracellular HDAC activity, cellular viability, metabolic activity, caspase activity, cell cycle progression, RNA and protein expression were analyzed. Results HDAC2 was found to be overexpressed in MB subgroups with poor prognosis (SHH, Group 3 and Group 4) compared to normal brain and the WNT subgroup. Inhibition of the enzymatic activity of the class I HDACs reduced metabolic activity, cell number, and viability in contrast to inhibition of class IIa HDACs. Increased sensitivity to HDACi was specifically observed in MYC amplified cells. Depletion of HDAC2 increased H4 acetylation and induced cell death. Simulation of clinical pharmacokinetics showed time-dependent on target activity that correlated with binding kinetics of HDACi compounds. Conclusions We conclude that HDAC2 is a valid drug target in patients with MYC amplified MB. HDACi should cover HDAC2 in their inhibitory profile and timing and dosing regimen in clinical trials should take binding kinetics of compounds into consideration.