Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue Sarcoma.
Anticancer Res
; 36(4): 1553-61, 2016 Apr.
Article
en En
| MEDLINE
| ID: mdl-27069131
ABSTRACT
BACKGROUND:
Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models. MATERIALS ANDMETHODS:
Anti-proliferative activity of eribulin was examined in vitro and in vivo in several human soft tissue sarcoma (STS) cell lines. To assess tumor blood perfusion and phenotypic changes, eribulin was investigated in a leiomyosarcoma xenograft and in vitro in liposarcoma and leiomyosarcoma cell lines.RESULTS:
Eribulin showed anti-proliferative activity in vitro against all six cell lines investigated, with 50% inhibitory concentration values of around 1 nmol/l, as well as significant antitumor activity against four xenografts in vivo. In addition, eribulin significantly enhanced tumor blood perfusion in xenografts and induced morphological changes and up-regulation of differentiation marker genes.CONCLUSION:
In pre-clinical models, eribulin showed anti-proliferative activity against a variety of histopathological subtypes of STS. Eribulin might also cause tumor vasculature remodeling to enhance tumor blood perfusion and induce tumor cell differentiation.Palabras clave
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Banco de datos:
MEDLINE
Asunto principal:
Sarcoma
/
Antimitóticos
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Furanos
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Cetonas
Límite:
Animals
/
Humans
Idioma:
En
Año:
2016
Tipo del documento:
Article