Selective repression of v-abl-encoded protein by N-methylisatin-beta-4',4'-diethylthiosemicarbazone and N-allylisatin-beta-4',4'-diallylthiosemicarbazone.
N-Methylisatin-beta-4',4'-diethylthiosemicarbazone (M-IBDET) and N-allylisatin-beta-4',4'-diallylthiosemicarbazone (A-IBDAT) selectively inhibited v-abl protein (P120), an oncogene product associated with tyrosine kinase activity. Concentrations of M-IBDET ranging between 0.17 and 0.64 microM and concentrations of A-IBDAT from 1.45 to 2.9 microM reduced tyrosine kinase activity significantly, whereas 0.64 microM M-IBDET and 2.9 microM A-IBDAT blocked P120 production. Cellular growth rate, protein production, and synthesis of p45 actin and p53 nuclear oncogene were not affected at these conditions. M-IBDET and A-IBDAT selectively suppress the v-abl oncogene as well as Moloney murine leukemia virus production.
Teitz
Y
Y
Department of Human Microbiology, Sackler School of Medicine, Tel Aviv University, Israel.
Ladizensky
E
E
Barko
N
N
Burstein
E
E
D000011:Abelson murine leukemia virus / Q000378:metabolism*; D000818:Animals; D002460:Cell Line; D004591:Electrophoresis, Polyacrylamide Gel; D007510:Isatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D008720:Methisazone / Q000031:analogs & derivatives* / Q000494:pharmacology; D051379:Mice; D008979:Moloney murine leukemia virus / Q000187:drug effects; D016374:Oncogene Proteins v-abl / Q000096:biosynthesis*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D013882:Thiosemicarbazones / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects
D016374:Oncogene Proteins v-abl; D013882:Thiosemicarbazones; C085307:N-allylisatin-beta-4',4'-diallylthiosemicarbazone; C022832:N-methylisatin beta-4',4'-diethylthiosemicarbazone; D007510:Isatin; D011505:Protein-Tyrosine Kinases; D008720:Methisazone