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 microM 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.
Laboratory for Environmental Toxicology and Chemistry, San Francisco State University, Tiburon, CA 94920, USA.
P I
PI
Bauer
E
E
Kirsten
G
G
Varadi
L J
LJ
Young
A
A
Hakam
J A
JA
Comstock
E
E
Kun
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002417:Cattle; D002471:Cell Transformation, Neoplastic / Q000187:drug effects*; D002478:Cells, Cultured; D003374:Coumarins / Q000494:pharmacology*; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects* / Q000473:pathology; D011905:Genes, ras; D006019:Glycolysis; D006801:Humans; D008024:Ligands; D008297:Male; D051379:Mice; D008819:Mice, Nude; D010641:Phenotype; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism*; D011471:Prostatic Neoplasms / Q000378:metabolism / Q000473:pathology*; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D003374:Coumarins; D008024:Ligands; C071383:5-iodo-6-amino-1,2-benzopyrone; D011065:Poly(ADP-ribose) Polymerases