Synthesis and biological activity of four kinds of reversed peptides.
We have synthesized four kinds of reversed peptides of various physiologically active peptides, which inhibit TNF (tumor necrosis factor) cytotoxicity, produce NGF (nerve growth factor), exert antimicrobial activity and inhibit cell attachment, respectively. They were examined for their biological activity in comparison with that of normal peptides, that is, naturally occurring peptides. The reversed peptides induce similar activities, but to a lesser extent than those of the normal peptides, respectively. These results indicate that there may be conformationally ambiguous binding in some of the naturally occurring ligand-protein interactions. This method may be useful as a tool to rapidly generate a novel lead peptide with the desired biological function from a naturally occurring active peptide.
Lie
B L
BL
Sagami Chemical Research Center, Kanagawa, Japan.
Iwahori
A
A
Sampe
R
R
Hirota
Y
Y
Tsubota
Y
Y
Yoshioka
H
H
Fuchita
S
S
Nakamura
N
N
Saita
R
R
Tunemoto
D
D
Numao
N
N
D000595:Amino Acid Sequence; D000818:Animals; D001419:Bacteria / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D051379:Mice; D008968:Molecular Conformation; D008969:Molecular Sequence Data; D009414:Nerve Growth Factors / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000633:toxicity
D009414:Nerve Growth Factors; D010455:Peptides; D014409:Tumor Necrosis Factor-alpha