A new endothelin C-terminal analogue IBDP 064 antagonizes endothelin-3-induced cell proliferation.
A series of C-terminal linear endothelin analogues were prepared and their activities in C6 rat glioma cell line were tested. Among the synthetic analogues, IBDP 064, Fmoc-Leu-Asp-Ile-Ile-Trp-OH, was the most potent and selective inhibitor of endothelin-3-induced cell proliferation. Its action was comparable with that of the previously described peptide IRL 1038, [Cys11-Cys15]-ET-1(11-21), an ETB specific inhibitor.
Sedo
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1st Department of Medical Chemistry and Biochemistry, 1st Medical Faculty, Charles University, Praha, Czech Republic.
Pegoraro
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Rovero
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Revoltella
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D000595:Amino Acid Sequence; D000818:Animals; D001798:Blood Proteins / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects*; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000494:pharmacology*; D005449:Fluorenes / Q000494:pharmacology*; D005910:Glioma; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000494:pharmacology*; D010446:Peptide Fragments / Q000494:pharmacology*; D051381:Rats; D017466:Receptors, Endothelin / Q000378:metabolism; D014407:Tumor Cells, Cultured
C095372:9-fluorenylmethoxycarbonyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophan-OH; D001798:Blood Proteins; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D005449:Fluorenes; D009842:Oligopeptides; D010446:Peptide Fragments; D017466:Receptors, Endothelin; C077420:Cys(11)-Cys(15)-endothelin-1 (11-21)