Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells

The HOX genes encode a family of transcription factors that have key roles in both development and malignancy. Disrupting the interaction between HOX proteins and their binding partner, PBX, has been shown to cause apoptotic cell death in a range of solid tumors. However, despite HOX proteins playin...

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Main Authors: Alharbi, Raed A., Pandha, Hardev S., Simpson, Guy R., Pettengell, Ruth, Poterlowicz, Krzysztof, Thompson, Alexander, Harrington, Kevin, El-Tanani, Mohamed, Morgan, Richard
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Published: Impact Journals 2017
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Online Access:https://eprints.nottingham.ac.uk/49748/
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author Alharbi, Raed A.
Pandha, Hardev S.
Simpson, Guy R.
Pettengell, Ruth
Poterlowicz, Krzysztof
Thompson, Alexander
Harrington, Kevin
El-Tanani, Mohamed
Morgan, Richard
author_facet Alharbi, Raed A.
Pandha, Hardev S.
Simpson, Guy R.
Pettengell, Ruth
Poterlowicz, Krzysztof
Thompson, Alexander
Harrington, Kevin
El-Tanani, Mohamed
Morgan, Richard
author_sort Alharbi, Raed A.
building Nottingham Research Data Repository
collection Online Access
description The HOX genes encode a family of transcription factors that have key roles in both development and malignancy. Disrupting the interaction between HOX proteins and their binding partner, PBX, has been shown to cause apoptotic cell death in a range of solid tumors. However, despite HOX proteins playing a particularly significant role in acute myeloid leukemia (AML), the relationship between HOX gene expression and patient survival has not been evaluated (with the exception of HOXA9), and the mechanism by which HOX/PBX inhibition induces cell death in this malignancy is not well understood. In this study, we show that the expression of HOXA5, HOXB2, HOXB4, HOXB9, and HOXC9, but not HOXA9, in primary AML samples is significantly related to survival. Furthermore, the previously described inhibitor of HOX/PBX dimerization, HXR9, is cytotoxic to both AML-derived cell lines and primary AML cells from patients. The mechanism of cell death is not dependent on apoptosis but instead involves a regulated form of necrosis referred to as necroptosis. HXR9-induced necroptosis is enhanced by inhibitors of protein kinase C (PKC) signaling, and HXR9 combined with the PKC inhibitor Ro31 causes a significantly greater reduction in tumor growth compared to either reagent alone.
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spelling nottingham-497482020-05-04T18:59:38Z https://eprints.nottingham.ac.uk/49748/ Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells Alharbi, Raed A. Pandha, Hardev S. Simpson, Guy R. Pettengell, Ruth Poterlowicz, Krzysztof Thompson, Alexander Harrington, Kevin El-Tanani, Mohamed Morgan, Richard The HOX genes encode a family of transcription factors that have key roles in both development and malignancy. Disrupting the interaction between HOX proteins and their binding partner, PBX, has been shown to cause apoptotic cell death in a range of solid tumors. However, despite HOX proteins playing a particularly significant role in acute myeloid leukemia (AML), the relationship between HOX gene expression and patient survival has not been evaluated (with the exception of HOXA9), and the mechanism by which HOX/PBX inhibition induces cell death in this malignancy is not well understood. In this study, we show that the expression of HOXA5, HOXB2, HOXB4, HOXB9, and HOXC9, but not HOXA9, in primary AML samples is significantly related to survival. Furthermore, the previously described inhibitor of HOX/PBX dimerization, HXR9, is cytotoxic to both AML-derived cell lines and primary AML cells from patients. The mechanism of cell death is not dependent on apoptosis but instead involves a regulated form of necrosis referred to as necroptosis. HXR9-induced necroptosis is enhanced by inhibitors of protein kinase C (PKC) signaling, and HXR9 combined with the PKC inhibitor Ro31 causes a significantly greater reduction in tumor growth compared to either reagent alone. Impact Journals 2017-08-07 Article PeerReviewed Alharbi, Raed A., Pandha, Hardev S., Simpson, Guy R., Pettengell, Ruth, Poterlowicz, Krzysztof, Thompson, Alexander, Harrington, Kevin, El-Tanani, Mohamed and Morgan, Richard (2017) Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells. Oncotarget, 8 (52). pp. 89566-89579. ISSN 1949-2553 acute myeloid leukemia HOX HXR9 necroptosis protein kinase C https://doi.org/10.18632/oncotarget.20023 doi:10.18632/oncotarget.20023 doi:10.18632/oncotarget.20023
spellingShingle acute myeloid leukemia
HOX
HXR9
necroptosis
protein kinase C
Alharbi, Raed A.
Pandha, Hardev S.
Simpson, Guy R.
Pettengell, Ruth
Poterlowicz, Krzysztof
Thompson, Alexander
Harrington, Kevin
El-Tanani, Mohamed
Morgan, Richard
Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title_full Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title_fullStr Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title_full_unstemmed Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title_short Inhibition of HOX/PBX dimer formation leads to necroptosis in acute myeloid leukemia cells
title_sort inhibition of hox/pbx dimer formation leads to necroptosis in acute myeloid leukemia cells
topic acute myeloid leukemia
HOX
HXR9
necroptosis
protein kinase C
url https://eprints.nottingham.ac.uk/49748/
https://eprints.nottingham.ac.uk/49748/
https://eprints.nottingham.ac.uk/49748/