Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

Gemma Di Pompo; Manuela Salerno; Dante Rotili; Sergio Valente; Clemens Zwergel; Sofia Avnet; Giovanna Lattanzi; Nicola Baldini; Antonello Mai

doi:10.1021/acs.jmedchem.5b00126

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

Gemma Di Pompo, Manuela Salerno, Dante Rotili, Sergio Valente, Clemens Zwergel, Sofia Avnet, Giovanna Lattanzi, Nicola Baldini, Antonello Mai

Istituti Ortopedici Rizzoli

Research output: Contribution to journal › Article

Abstract

Musculoskeletal sarcomas are aggressive malignancies of bone and soft tissues often affecting children and adolescents. Histone deacetylase inhibitors (HDACi) have been proposed to counteract cancer stem cells (CSCs) in solid neoplasms. When tested in human osteosarcoma, rhabdomyosarcoma, and Ewing's sarcoma stem cells, the new HDACi MC1742 (1) and MC2625 (2) increased acetyl-H3 and acetyl-tubulin levels and inhibited CSC growth by apoptosis induction. At nontoxic doses, 1 promoted osteogenic differentiation. Further investigation with 1 will be done in preclinical sarcoma models.

Original language	English
Pages (from-to)	4073-4079
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	58
Issue number	9
DOIs	https://doi.org/10.1021/acs.jmedchem.5b00126
Publication status	Published - May 14 2015

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery
Medicine(all)

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10.1021/acs.jmedchem.5b00126

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Di Pompo, G., Salerno, M., Rotili, D., Valente, S., Zwergel, C., Avnet, S., Lattanzi, G., Baldini, N., & Mai, A. (2015). Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. Journal of Medicinal Chemistry, 58(9), 4073-4079. https://doi.org/10.1021/acs.jmedchem.5b00126

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. / Di Pompo, Gemma; Salerno, Manuela; Rotili, Dante; Valente, Sergio; Zwergel, Clemens; Avnet, Sofia ; Lattanzi, Giovanna ; Baldini, Nicola; Mai, Antonello.

In: Journal of Medicinal Chemistry, Vol. 58, No. 9, 14.05.2015, p. 4073-4079.

Research output: Contribution to journal › Article

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