Antitumor effect of methylglyoxal bis(3-aminopropylamidinohydrazone), a new inhibitor of S-adenosylmethionine and ornithine decarboxylases, on human erythroid leukemia K562 cells.
Methylglyoxal bis(3-aminopropylamidinohydrazone (MGBA) inhibited S-adenosylmethionine decarboxylase (AdoMetDC) activity competitively with S-adenosylmethionine (AdoMet), showing a Ki value of 2.60 x 10(-5) M. It also inhibited ornithine decarboxylase competitively with ornithine, showing a Ki value of 3.80 x 10(-5) M. MGBA inhibited the growth of human erythroid leukemia K562 cells. Putrescine, spermidine, and spermine concentrations in MGBA-treated cells were depressed to 19%, 36%, and 66% of the values of control cells, respectively.
Hibasami
H
H
Department of Biochemistry, Mie University School of Medicine, Japan.
Tsukada
T
T
Maekawa
S
S
Sakurai
M
M
Shirakawa
S
S
Nakashima
K
K
D012437:Adenosylmethionine Decarboxylase / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D000970:Antineoplastic Agents; D002262:Carboxy-Lyases / Q000037:antagonists & inhibitors*; D002455:Cell Division / Q000187:drug effects; D004790:Enzyme Induction / Q000187:drug effects; D006801:Humans; D008935:Mitoguazone / Q000031:analogs & derivatives* / Q000494:pharmacology; D065108:Ornithine Decarboxylase Inhibitors; D011073:Polyamines / Q000378:metabolism; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D065108:Ornithine Decarboxylase Inhibitors; D011073:Polyamines; C057056:methylglyoxal bis(3-aminopropylamidinohydrazone); D002262:Carboxy-Lyases; D012437:Adenosylmethionine Decarboxylase; D008935:Mitoguazone