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Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.

作者信息

Herrmann Harald, Blatt Katharina, Shi Junwei, Gleixner Karoline V, Cerny-Reiterer Sabine, Müllauer Leonhard, Vakoc Christopher R, Sperr Wolfgang R, Horny Hans-Peter, Bradner James E, Zuber Johannes, Valent Peter

机构信息

Ludwig Boltzmann Cluster Oncology, Vienna, Austria.

出版信息

Oncotarget. 2012 Dec;3(12):1588-99. doi: 10.18632/oncotarget.733.


DOI:10.18632/oncotarget.733
PMID:23249862
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3681497/
Abstract

Acute myeloid leukemia (AML) is a life-threatening stem cell disease characterized by uncontrolled proliferation and accumulation of myeloblasts. Using an advanced RNAi screen-approach in an AML mouse model we have recently identified the epigenetic 'reader' BRD4 as a promising target in AML. In the current study, we asked whether inhibition of BRD4 by a small-molecule inhibitor, JQ1, leads to growth-inhibition and apoptosis in primary human AML stem- and progenitor cells. Primary cell samples were obtained from 37 patients with freshly diagnosed AML (n=23) or refractory AML (n=14). BRD4 was found to be expressed at the mRNA and protein level in unfractionated AML cells as well as in highly enriched CD34⁺/CD38⁻ and CD34⁺/CD38⁺ stem- and progenitor cells in all patients examined. In unfractionated leukemic cells, submicromolar concentrations of JQ1 induced major growth-inhibitory effects (IC₅₀ 0.05-0.5 µM) in most samples, including cells derived from relapsed or refractory patients. In addition, JQ1 was found to induce apoptosis in CD34+/CD38⁻ and CD34⁺/CD38⁺ stem- and progenitor cells in all donors examined as evidenced by combined surface/Annexin-V staining. Moreover, we were able to show that JQ1 synergizes with ARA-C in inducing growth inhibition in AML cells. Together, the BRD4-targeting drug JQ1 exerts major anti-leukemic effects in a broad range of human AML subtypes, including relapsed and refractory patients and all relevant stem- and progenitor cell compartments, including CD34⁺/CD38⁻ and CD34⁺/CD38⁺ AML cells. These results characterize BRD4-inhibition as a promising new therapeutic approach in AML which should be further investigated in clinical trials.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/aab460664ca8/oncotarget-03-1588-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/7addb90ba431/oncotarget-03-1588-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/1d650918bc34/oncotarget-03-1588-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/c93dd67e5f65/oncotarget-03-1588-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/aab460664ca8/oncotarget-03-1588-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/7addb90ba431/oncotarget-03-1588-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/1d650918bc34/oncotarget-03-1588-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/c93dd67e5f65/oncotarget-03-1588-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/baf9/3681497/aab460664ca8/oncotarget-03-1588-g004.jpg

相似文献

[1]
Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.

Oncotarget. 2012-12

[2]
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[3]
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[6]
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[7]
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[10]
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[7]
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[8]
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[9]
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[10]
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本文引用的文献

[1]
Cancer stem cell definitions and terminology: the devil is in the details.

Nat Rev Cancer. 2012-10-11

[2]
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N Engl J Med. 2012-8-16

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Essential role for telomerase in chronic myeloid leukemia induced by BCR-ABL in mice.

Oncotarget. 2012-3

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The Hsp32 inhibitors SMA-ZnPP and PEG-ZnPP exert major growth-inhibitory effects on D34+/CD38+ and CD34+/CD38- AML progenitor cells.

Curr Cancer Drug Targets. 2012-1

[8]
Chronic myeloid leukemia stem cells in the era of targeted therapies: resistance, persistence and long-term dormancy.

Oncotarget. 2011-9

[9]
Stem cell gene expression programs influence clinical outcome in human leukemia.

Nat Med. 2011-8-28

[10]
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.

Nature. 2011-8-3

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