Conformational Prerequisites for the in vitro Inhibition of Cholate Uptake in Hepatocytes by Cyclic Analogues of Antamanide and Somatostatin

Constitution and conformation determine the biological activity of a peptide, as demonstrated by comparative investigations of the inhibition of cholate uptake in liver cells by somatostatin, antamanide, cyclolinopeptide A and 1 and 2. The crystal structure of 1 is the same as that of 2 over a wide...

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Veröffentlicht in:Angewandte Chemie International Edition 1986-11, Vol.25 (11), p.997-999
Hauptverfasser: Kessler, Horst, Klein, Mechtild, Müller, Arndt, Wagner, Klaus, Bats, Jan Willem, Ziegler, Kornelia, Frimmer, Max
Format: Artikel
Sprache:eng
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Zusammenfassung:Constitution and conformation determine the biological activity of a peptide, as demonstrated by comparative investigations of the inhibition of cholate uptake in liver cells by somatostatin, antamanide, cyclolinopeptide A and 1 and 2. The crystal structure of 1 is the same as that of 2 over a wide range and both react strongly cytoprotectively.
ISSN:0570-0833
1521-3773
DOI:10.1002/anie.198609971