Reversion of malignant phenotype by 5-iodo-6-amino-1,2-benzopyrone a non-covalently binding ligand of poly(ADP-ribose) polymerase

A non-covalently binding inhibitory ligand of poly(ADP-ribose) polymerase, 5-iodo-6-amino-1,2-benzopyrone, when incubated at 5–600 μM external concentration with an E-ras-transformed tumorigenic cell line or with human prostatic carcinoma cells for 40 to 60 days converts both cancer cells to a non-t...

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Veröffentlicht in:	Biochimie 1995, Vol.77 (5), p.374-377
Hauptverfasser:	Bauer, P.I., Kirsten, E., Varadi, G., Young, L.J.T., Hakam, A., Comstock, J.A., Kun, E.
Format:	Artikel
Sprache:	eng
Schlagworte:	5-iodo-6-amino-1,2-benzopyrone Animals Antineoplastic Agents - pharmacology Cattle Cell Transformation, Neoplastic - drug effects Cells, Cultured Coumarins - pharmacology DU 145 cells E-ras 20 cells Endothelium, Vascular - cytology Endothelium, Vascular - drug effects Endothelium, Vascular - pathology Genes, ras Glycolysis Humans Ligands Male malignant phenotype Mice Mice, Nude Phenotype poly(ADP-ribose) polymerase Poly(ADP-ribose) Polymerases - metabolism Prostatic Neoplasms - metabolism Prostatic Neoplasms - pathology Transplantation, Heterologous Tumor Cells, Cultured
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Beschreibung
Zusammenfassung:	A non-covalently binding inhibitory ligand of poly(ADP-ribose) polymerase, 5-iodo-6-amino-1,2-benzopyrone, when incubated at 5–600 μM external concentration with an E-ras-transformed tumorigenic cell line or with human prostatic carcinoma cells for 40 to 60 days converts both cancer cells to a non-tumorigenic phenotype that is characterized by drastic changes in cell morphology, absence of tumorigenicity in nude mice, and a high rate of aerobic glycolysis.
ISSN:	0300-9084 1638-6183
DOI:	10.1016/0300-9084(96)88149-1