首页> 外文期刊>Journal of Medicinal Chemistry >Novel Histone Deacetylase Inhibitors Induce Growth Arrest, Apoptosis, and Differentiation in Sarcoma Cancer Stem Cells
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Novel Histone Deacetylase Inhibitors Induce Growth Arrest, Apoptosis, and Differentiation in Sarcoma Cancer Stem Cells

机译:新型组蛋白脱乙酰基酶抑制剂在肉瘤癌干细胞中诱导生长停滞,凋亡和分化。

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摘要

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 prolinical sarcoma model.
机译:肌肉骨骼肉瘤是经常侵袭儿童和青少年的骨骼和软组织的恶性肿瘤。已提出组蛋白脱乙酰基酶抑制剂(HDACi)来抵抗固体肿瘤中的癌症干细胞(CSC)。当在人骨肉瘤,横纹肌肉瘤和尤因氏肉瘤干细胞中进行测试时,新的HDACi MC1742(1)和MC2625(2)可以通过诱导细胞凋亡来提高乙酰H3和乙酰微管蛋白水平并抑制CSC生长。在无毒剂量下,1促进成骨分化。在临床肉瘤模型中将对1做进一步的研究。

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