Enhancement of cytotoxic activity by synthesis of peptide multimeric forms.
Synthesis of four multimeric H-Lys-His-His-Arg-Lys-Lys-His-Arg-Lys-Arg-Lys-His-His-Lys-Arg-Lys-oH peptides containing two, four, eight and sixteen branches was carried out by solid phase utilizing a lysine core matrix. These multimeric peptides enhanced activity by inhibiting the colony-forming ability of HeLa cells, from twenty-four to fifty-six times in comparison with the monomeric form. Unexpectedly the peptide with only two-branched sequences showed the highest inhibitory activity.
Chillemi
F
F
Dipartimento di Chimica Organica e Industriale, Università di Milano, Italy.
Francescato
P
P
Bossa
R
R
Fraccari
A
A
Galatulas
I
I
D000595:Amino Acid Sequence; D002455:Cell Division / Q000187:drug effects; D006131:Growth Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D008239:Lysine / Q000737:chemistry; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D006131:Growth Inhibitors; D009842:Oligopeptides; D008239:Lysine