Investigations on the antitumor effect and mutagenicity of alpha-MSH fragments containing melphalan.
alpha-MSH fragments containing melphalan were tested in vivo on L1210 leukemia and on human amelanotic melanoma xenograft in mice and in vitro on human amelanotic melanoma cell lines. The compounds exhibit significant antitumor activity, but no selectivity in targeting of melanoma can be achieved. There is a difference between melphalan and the melphalyl-peptide in their action on protein synthesis. The peptide derivatives also are less mutagenic than melphalan, according to the SCE assay, furnishing further evidence for the positive effect of natural carrier molecules.
Süli-Vargha
H
H
Research Group for Peptide Chemistry, Hungarian Academy of Science, Budapest.
Jeney
A
A
Kopper
L
L
Oláh
J
J
Lapis
K
K
Botyánszki
J
J
Csukás
I
I
Gyövári
B
B
Medzihradszky
K
K
D000595:Amino Acid Sequence; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001001:Anura; D005260:Female; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D008558:Melphalan / Q000494:pharmacology*; D051379:Mice; D008969:Molecular Sequence Data; D014442:Monophenol Monooxygenase / Q000378:metabolism; D009152:Mutagenicity Tests; D009368:Neoplasm Transplantation; D010455:Peptides / Q000494:pharmacology*; D012854:Sister Chromatid Exchange / Q000187:drug effects; D012867:Skin / Q000187:drug effects; D000521:alpha-MSH / Q000494:pharmacology*
D000970:Antineoplastic Agents; D010455:Peptides; D000521:alpha-MSH; D014442:Monophenol Monooxygenase; D008558:Melphalan