The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells

The central role of the control of apoptosis in the pathophysiology of Philadelphia chromosome-negative myeloproliferative neoplasms has recently been reinforced in genetic and pharmacological studies. The inhibitor of apoptosis protein family has eight members and plays an important role in apoptos...

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Main Authors: Jorge Antonio Elias Godoy Carlos, Keli Lima, Eduardo Magalhães Rego, Leticia Veras Costa-Lotufo, João Agostinho Machado-Neto
Format: Article
Language:English
Published: Elsevier 2024-12-01
Series:Hematology, Transfusion and Cell Therapy
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Online Access:http://www.sciencedirect.com/science/article/pii/S2531137924003092
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author Jorge Antonio Elias Godoy Carlos
Keli Lima
Eduardo Magalhães Rego
Leticia Veras Costa-Lotufo
João Agostinho Machado-Neto
author_facet Jorge Antonio Elias Godoy Carlos
Keli Lima
Eduardo Magalhães Rego
Leticia Veras Costa-Lotufo
João Agostinho Machado-Neto
author_sort Jorge Antonio Elias Godoy Carlos
collection DOAJ
description The central role of the control of apoptosis in the pathophysiology of Philadelphia chromosome-negative myeloproliferative neoplasms has recently been reinforced in genetic and pharmacological studies. The inhibitor of apoptosis protein family has eight members and plays an important role in apoptosis, with the most studied being survivin (BIRC5) and X-linked inhibitor of apoptosis (XIAP). YM155 is a small molecule with antineoplastic potential that has been described as a suppressant of survivin and XIAP. In the present study, BIRC5 expression was significantly increased in primary myelofibrosis patients compared to healthy donors. On the other hand, XIAP expression was reduced in myeloproliferative neoplasms patients. In JAK2V617F cells, YM155 reduces cell viability and autonomous clonal growth and induces apoptosis, cell cycle arrest, and autophagy. HEL cells that show greater malignancy are more sensitive to the drug than SET2 cells. In the molecular scenario, YM155 modulates apoptosis-, cell cycle-, DNA damage- and autophagy-related genes. Protein expression analysis corroborates the observed cellular phenotype and exploratory gene expression findings. In summary, our results indicate that survivin/BIRC5 and XIAP are differently expressed in myeloproliferative neoplasms and YM155 has multiple antineoplastic effects on JAK2V617F cells suggesting that inhibitor of apoptosis proteins may be a target for pharmacological interventions in the treatment of these diseases.
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spelling doaj-art-db6927c88e534f198576c1dbfa2ffccd2024-12-21T04:29:37ZengElsevierHematology, Transfusion and Cell Therapy2531-13792024-12-0146S217S227The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cellsJorge Antonio Elias Godoy Carlos0Keli Lima1Eduardo Magalhães Rego2Leticia Veras Costa-Lotufo3João Agostinho Machado-Neto4Department of Pharmacology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, BrazilDepartment of Pharmacology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, Brazil; Laboratory of Medical Investigation in Pathogenesis and Targeted Therapy in Onco-Immuno-Hematology (LIM-31), Department of Internal Medicine, Hematology Division, Medical School, University of São Paulo, São Paulo, BrazilLaboratory of Medical Investigation in Pathogenesis and Targeted Therapy in Onco-Immuno-Hematology (LIM-31), Department of Internal Medicine, Hematology Division, Medical School, University of São Paulo, São Paulo, BrazilDepartment of Pharmacology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, BrazilDepartment of Pharmacology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, Brazil; Corresponding author at: Department of Pharmacology, Institute of Biomedical Sciences of University of São Paulo, Av. Prof. Lineu Prestes, 1524, CEP: 05508-900, São Paulo, SP, Brazil.The central role of the control of apoptosis in the pathophysiology of Philadelphia chromosome-negative myeloproliferative neoplasms has recently been reinforced in genetic and pharmacological studies. The inhibitor of apoptosis protein family has eight members and plays an important role in apoptosis, with the most studied being survivin (BIRC5) and X-linked inhibitor of apoptosis (XIAP). YM155 is a small molecule with antineoplastic potential that has been described as a suppressant of survivin and XIAP. In the present study, BIRC5 expression was significantly increased in primary myelofibrosis patients compared to healthy donors. On the other hand, XIAP expression was reduced in myeloproliferative neoplasms patients. In JAK2V617F cells, YM155 reduces cell viability and autonomous clonal growth and induces apoptosis, cell cycle arrest, and autophagy. HEL cells that show greater malignancy are more sensitive to the drug than SET2 cells. In the molecular scenario, YM155 modulates apoptosis-, cell cycle-, DNA damage- and autophagy-related genes. Protein expression analysis corroborates the observed cellular phenotype and exploratory gene expression findings. In summary, our results indicate that survivin/BIRC5 and XIAP are differently expressed in myeloproliferative neoplasms and YM155 has multiple antineoplastic effects on JAK2V617F cells suggesting that inhibitor of apoptosis proteins may be a target for pharmacological interventions in the treatment of these diseases.http://www.sciencedirect.com/science/article/pii/S2531137924003092Myeloproliferative neoplasmsInhibitor of apoptosis proteinsSurvivingXIAPYM155
spellingShingle Jorge Antonio Elias Godoy Carlos
Keli Lima
Eduardo Magalhães Rego
Leticia Veras Costa-Lotufo
João Agostinho Machado-Neto
The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
Hematology, Transfusion and Cell Therapy
Myeloproliferative neoplasms
Inhibitor of apoptosis proteins
Surviving
XIAP
YM155
title The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
title_full The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
title_fullStr The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
title_full_unstemmed The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
title_short The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells
title_sort survivin xiap suppressant ym155 impairs clonal growth and induces apoptosis in jak2v617f cells
topic Myeloproliferative neoplasms
Inhibitor of apoptosis proteins
Surviving
XIAP
YM155
url http://www.sciencedirect.com/science/article/pii/S2531137924003092
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