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PMID: 24098593 Published · epublish English Journal Article Research Support, Non-U.S. Gov't

PD-0332991, a CDK4/6 inhibitor, significantly prolongs survival in a genetically engineered mouse model of brainstem glioma.

PloS one ·Vol. 8 ·No. 10 ·2013-00-00 ·Pages e77639

Barton KL, Misuraca K, Cordero F, Dobrikova E, Min HD, Gromeier M, Kirsch DG, Becher OJ

Abstract

Diffuse intrinsic pontine glioma (DIPG) is an incurable tumor that arises in the brainstem of children. To date there is not a single approved drug to effectively treat these tumors and thus novel therapies are desperately needed. Recent studies suggest that a significant fraction of these tumors contain alterations in cell cycle regulatory genes including amplification of the D-type cyclins and CDK4/6, and less commonly, loss of Ink4a-ARF leading to aberrant cell proliferation. In this study, we evaluated the therapeutic approach of targeting the cyclin-CDK-Retinoblastoma (Rb) pathway in a genetically engineered PDGF-B-driven brainstem glioma (BSG) mouse model. We found that PD-0332991 (PD), a CDK4/6 inhibitor, induces cell-cycle arrest in our PDGF-B; Ink4a-ARF deficient model both in vitro and in vivo. By contrast, the PDGF-B; p53 deficient model was mostly resistant to treatment with PD. We noted that a 7-day treatment course with PD significantly prolonged survival by 12% in the PDGF-B; Ink4a-ARF deficient BSG model. Furthermore, a single dose of 10 Gy radiation therapy (RT) followed by 7 days of treatment with PD increased the survival by 19% in comparison to RT alone. These findings provide the rationale for evaluating PD in children with Ink4a-ARF deficient gliomas.

MeSH Terms
Animals Antineoplastic Agents/pharmacology Brain Stem Neoplasms/genetics,mortality,pathology,therapy Cell Cycle Checkpoints/drug effects,radiation effects Cell Proliferation/drug effects,radiation effects Cyclin-Dependent Kinase 4/antagonists & inhibitors,genetics,metabolism Cyclin-Dependent Kinase 6/antagonists & inhibitors,genetics,metabolism Cyclin-Dependent Kinase Inhibitor p16/deficiency,genetics Disease Models, Animal Drug Administration Schedule Gamma Rays Gene Expression Regulation, Neoplastic/drug effects,radiation effects Glioma/genetics,mortality,pathology,therapy Mice Oncogene Proteins, Fusion/deficiency,genetics Piperazines/pharmacology Proto-Oncogene Proteins c-sis/genetics,metabolism Pyridines/pharmacology Retinoblastoma Protein/genetics,metabolism Signal Transduction Survival Analysis
Chemicals
Antineoplastic Agents Cdkn2a protein, mouse Cyclin-Dependent Kinase Inhibitor p16 Oncogene Proteins, Fusion Piperazines Proto-Oncogene Proteins c-sis Pyridines Retinoblastoma Protein Cdk4 protein, mouse Cdk6 protein, mouse Cyclin-Dependent Kinase 4 Cyclin-Dependent Kinase 6 palbociclib
Authors & Affiliations
8 authors, click to expand affiliations / ORCID
Barton Kelly L
Department of Pediatrics, Duke University, Durham, North Carolina, United States of America ; Preston Robert Tisch Brain Tumor Center, Duke University, Durham, North Carolina, United States of America.
Misuraca Katherine
Cordero Francisco
Dobrikova Elena
Min Hooney D
Gromeier Matthias
Kirsch David G
Becher Oren J
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Article Info
Journal
PloS one
Abbr.
PLoS One
ISSN
1932-6203
Published
2013-00-00
Epub
2013-00-02
Pages
e77639
Language
English
Region
United States
NLM ID
101285081
PMCID
PMC3788718
Subset
IM
Grants
NIAID NIH HHS · K02 AI093866 · United States
NCI NIH HHS · R01 CA124756 · United States
NICHD NIH HHS · T32 HD040372 · United States
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