Musculoskeletal sarcomas are aggressive malignan-cies of bone and soft tissues often affecting children andadolescents. Histone deacetylase inhibitors (HDACi) have beenproposed to counteract cancer stem cells (CSCs) in solidneoplasms. When tested in human osteosarcoma, rhabdomyosar-coma, and Ewing’s sarcoma stem cells, the new HDACi MC1742(1) and MC2625 (2) increased acetyl-H3 and acetyl-tubulin levelsand inhibited CSC growth by apoptosis induction. At nontoxicdoses,1promoted osteogenic differentiation. Further investigationwith1will be done in preclinical sarcoma models.
Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells / G., Di Pompo; M., Salerno; Rotili, Dante; Valente, Sergio; Zwergel, Clemens; S., Avnet; G., Lattanzi; N., Baldini; Mai, Antonello. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 58:9(2015), pp. 4073-4079. [10.1021/acs.jmedchem.5b00126]
Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells
ROTILI, Dante;VALENTE, Sergio;ZWERGEL, CLEMENS;MAI, Antonello
2015
Abstract
Musculoskeletal sarcomas are aggressive malignan-cies of bone and soft tissues often affecting children andadolescents. Histone deacetylase inhibitors (HDACi) have beenproposed to counteract cancer stem cells (CSCs) in solidneoplasms. When tested in human osteosarcoma, rhabdomyosar-coma, and Ewing’s sarcoma stem cells, the new HDACi MC1742(1) and MC2625 (2) increased acetyl-H3 and acetyl-tubulin levelsand inhibited CSC growth by apoptosis induction. At nontoxicdoses,1promoted osteogenic differentiation. Further investigationwith1will be done in preclinical sarcoma models.| File | Dimensione | Formato | |
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