Conformational study of a series of somatostatin analogues with antitumor and/or GH inhibitory activity.
A series of somatostatin analogues with varying activities have been studied by 1H NMR in CD3OH at low temperature in order to find a possible structural explanation for the differentiation of biological activities. In somatostatin analogues with GH release inhibitory activity a beta-turn/beta-sheet backbone conformation is present, which is shown to be characteristic of somatostatin-derived peptides exhibiting this biological activity. On the other hand, among the analogues with antitumor activity, a deviation from these typical structural features is clearly observed, but not general conformational model can be proposed.
Jaspers
H
H
Department of Organic Chemistry, Free University of Brussels, Belgium.
Horvåth
A
A
Mezö
I
I
Kéri
G
G
Van Binst
G
G
D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D003080:Cold Temperature; D003903:Deuterium; D013006:Growth Hormone / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D000432:Methanol; D008969:Molecular Sequence Data; D011487:Protein Conformation; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013816:Thermodynamics
D000970:Antineoplastic Agents; D013004:Somatostatin; D013006:Growth Hormone; D003903:Deuterium; D000432:Methanol