title: Structural requirements for galanin interaction with receptors from pancreatic beta cells and from brain tissue of the rat.
abstract: The binding activity of several galanin fragments and analogs was measured on specific receptors present in rat brain and the rat pancreatic beta cell line Rin m 5F. In both tissues it was observed that: 1) galanin(3-29), galanin(10-29) and [Ile2]-galanin were ineffective for inhibiting [125I] galanin binding and 2) active peptides had the following rank order of potency: galanin(1-29) greater than [Ac-Trp2]-galanin(2-29) greater than galanin(2-29) greater than galanin(1-15) greater than [Phe2]-galanin greater than [Tyr2]-galanin. It was concluded that the N-terminal portion of galanin is very important for interaction with central or peripheral receptors. The aromatic amino acid in position 2 (Trp in native galanin) plays a crucial role.
authors: INSERM U178, Unité de Recherches sur la Différenciation et la Neuroendocrinologie de Cellules Digestives, Bâtiment INSERM, Villejuif, France.
authors: I
authors: I
authors: Lagny-Pourmir
authors: A M
authors: AM
authors: Lorinet
authors: N
authors: N
authors: Yanaihara
authors: M
authors: M
authors: Laburthe
mesh_terms: D000596:Amino Acids / Q000032:analysis; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects*; D002460:Cell Line; D002478:Cells, Cultured; D019004:Galanin; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007515:Islets of Langerhans / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D008566:Membranes / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D010446:Peptide Fragments / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D044088:Receptors, Galanin; D011964:Receptors, Gastrointestinal Hormone / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D007457:Iodine Radioisotopes; D009419:Nerve Tissue Proteins; D010446:Peptide Fragments; D010455:Peptides; D044088:Receptors, Galanin; D011964:Receptors, Gastrointestinal Hormone; D019004:Galanin