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Título
Irvalec inserts into the plasma membrane causing rapid loss of integrity and necrotic cell death in tumor cells
Autor
Año del Documento
2011
Editorial
Public Library of Science
Descripción
Producción Científica
Documento Fuente
PLoS ONE, 2011, vol. 6, n. 4. 13 p.
Abstract
Irvalec is a marine-derived antitumor agent currently undergoing phase II clinical trials. In vitro, Irvalec induces a rapid loss of membrane integrity in tumor cells, accompanied of a significant Ca2+ influx, perturbations of membrane conductivity, severe swelling and the formation of giant membranous vesicles. All these effects are not observed in Irvalec-resistant cells, or are significantly delayed by pretreating the cells with Zn2+. Using fluorescent derivatives of Irvalec it was demonstrated that the compound rapidly interacts with the plasma membrane of tumor cells promoting lipid bilayer restructuration. Also, FRET experiments demonstrated that Irvalec molecules localize in the cell membrane close enough to each other as to suggest that the compound could self-organize, forming supramolecular structures that likely trigger cell death by necrosis through the disruption of membrane integrity.
Palabras Clave
Antitumor drugs
Fármacos antitumorales
Plasma membrane
Membrana plasmática
ISSN
1932-6203
Revisión por pares
SI
Patrocinador
Ministerio de Ciencia, Innovación y Universidades (grants SAF2007-65868 , SAF2010-14916, FIS RD06/0014/0006, PIF200680F0023, S-BIO-0260/2006 and CTQ 2009-12412)
Version del Editor
Propietario de los Derechos
© 2011 Public Library of Science
Idioma
eng
Tipo de versión
info:eu-repo/semantics/publishedVersion
Derechos
openAccess
Collections
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