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Novel galanin receptor ligands

Academic Article
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Overview

authors

  • Pooga, M.
  • Jureus, A.
  • Rezaei, K.
  • Hasanvan, H.
  • Saar, K.
  • Kask, K.
  • Kjellen, P.
  • Land, T.
  • Halonen, J.
  • Maeorg, U.
  • Uri, A.
  • Solyom, S.
  • Bartfai, Tamas
  • Langel, Ülo

publication date

  • January 1998

journal

  • Journal of Peptide Research  Journal

abstract

  • Galanin is a neuroendocrine peptide which is 29/30 amino acids in length and is recognised by G-protein-coupled central nervous system receptors via its N-terminus. We synthesised several galanin receptor ligands and fragments around C-terminal extensions of galanin(1-13) to yield chimeric peptides with C-terminals corresponding to bioactive peptides like bradykinin(2-9), mastoparan, neuropeptide Y(25-36) or substance P(5-11), respectively. We also synthesised short galanin analogs in which galanin(1-13) was C-terminally elongated with Lys14; different pharmacologically active small molecules were then attached to the epsilon-amino group of Lys14. Several cysteine-substituted linear and ring closed analogs of galanin(1-9) and galanin(1-16) were also synthesised. The equilibrium binding constants for these peptides at hypothalamic galanin receptors were determined and found in the subnanomolar to micromolar range. The large number of peptides and their binding affinities presented here permit structure-activity relationship analysis of peptide-type ligands to galanin receptors.

subject areas

  • Amino Acid Sequence
  • Animals
  • Ligands
  • Male
  • Molecular Sequence Data
  • Peptides
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone
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Research

keywords

  • binding
  • chimeric peptide
  • galanin
  • galanin receptor
  • hypothalamus
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Identity

International Standard Serial Number (ISSN)

  • 1397-002X

PubMed ID

  • 9495593
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Additional Document Info

start page

  • 65

end page

  • 74

volume

  • 51

issue

  • 1

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