English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/124432
COMPARTIR / IMPACTO:
Estadísticas
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Título

The activity of a novel mithramycin analog is related to its binding to DNA, cellular accumulation, and inhibition of Sp1-driven gene transcription

AutorFernández-Guizán, Azahara; Mansilla, Sylvia ; Barceló, Francisca; Vizcaíno, Carolina ; Núñez, Luz-Elena; Morís, Francisco; González, Segundo; Portugal, José
Palabras claveCell Uptake
DNA-binding
Mithramycin
Ovarian cancer
Transcription
Fecha de publicación5-ago-2014
EditorElsevier
CitaciónChemico-Biological Interactions 219: 123-132 (2014)
ResumenDIG-MSK (demycarosyl-3D-β-d-digitoxosyl-mithramycin SK) is a recently isolated compound of the mithramycin family of antitumor antibiotics, which includes mithramycin A (MTA) and mithramycin SK (MSK). Here, we present evidence that the binding of DIG-MSK to DNA shares the general features of other mithramycins such as the preference for C/G-rich tracts, but there are some differences in the strength of binding and the DNA sequence preferentially recognized by DIG-MSK. We aimed at gaining further insights into the DIG-MSK mechanism of action by direct comparison with the effects of the parental MTA. Similar to MTA, MSK and DIG-MSK accumulated rapidly in A2780, IGROV1 and OVCAR3 human ovarian cancer cell lines, and DIG-MSK was a potent inhibitor of both basal and induced expression of an Sp1-driven luciferase vector. This inhibitory activity was confirmed for the endogenous Sp1 gene and a set of Sp-responsive genes, and compared to that of MTA and MSK. Furthermore, DIG-MSK was stronger than MTA as inhibitor of Sp3-driven transcription and endogenous Sp3 gene expression. Differences in the effects of MTA, MSK and DIG-MSK on gene expression may have a large influence on their biological activities. © 2014 Elsevier Ltd. All rights reserved.
Versión del editorhttp://dx.doi.org/10.1016/j.cbi.2014.05.019
URIhttp://hdl.handle.net/10261/124432
DOI10.1016/j.cbi.2014.05.019
Identificadoresdoi: 10.1016/j.cbi.2014.05.019
issn: 1872-7786
Aparece en las colecciones: (IBMB) Artículos
Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
ChemBiolInter(2014).pdf1,03 MBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo
 

Artículos relacionados:


NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.