Structural requirement for galanin action in the pancreatic beta cell line Rin m 5F.
Galanin fragments were tested for their ability to alter forskolin-stimulated cyclic AMP production and insulin release from Rin m 5F cells. Galanin and its fragments inhibited both events with the following potencies: Gal-(1-29) greater than N-AcGal-(2-29) greater than Gal-(2-29) greater than Gal-(1-15). In contrast, Gal-(3-29), Gal-(10-29) and [Ile2]Gal were inactive. [Phe2]- and [Tyr2]Gal were moderately effective. We conclude that the N-terminal portion of galanin (in particular the aromatic amino acid in position 2) is crucial for activity.
Amiranoff
B
B
INSERM U178, Unité de Recherches sur la Différenciation et la Neuroendocrinologie de Cellules Digestives, Villejuif, France.
Lorinet
A M
AM
Yanaihara
N
N
Laburthe
M
M
D000818:Animals; D002460:Cell Line; D000242:Cyclic AMP / Q000378:metabolism; D019004:Galanin; D007328:Insulin / Q000378:metabolism; D007515:Islets of Langerhans / Q000187:drug effects / Q000378:metabolism*; D010446:Peptide Fragments / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013552:Swine
D007328:Insulin; D010446:Peptide Fragments; D010455:Peptides; D019004:Galanin; D000242:Cyclic AMP