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

Autori

Di Pompo G, Salerno M, Rotili D, Valente S, Zwergel C, Avnet S, Lattanzi G, Baldini N, Mai A.

Riferimenti

JOURNAL OF MEDICINAL CHEMISTRY 58(9) 4073-4079, 2015

Autori CNR

LATTANZI

Moduli

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.

Link all articolo

http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00126

Parole Chiave

Note

Indietro


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