Novel peptide agonists, favoring galanin receptor type 2 over galanin receptor type 1 and 3
2009 (English)In: The FEBS Journal, ISSN 1742-464X, E-ISSN 1742-4658, Vol. 276, 164-164 p.Article in journal, Meeting abstract (Refereed) Published
The galanin peptide family and its three receptors have with compelling evidence been implicated in a variety of human disorders. The co-localization with other neuromodulators and the distinct up-regulation during and after pathological disturbances has drawn attention to this neuropeptide family although, so far, no therapeutics have emerged past the animal model stage. In the current study we present data on receptor binding and functional response from novel galanin receptor type 2 (GalR2) selective chimeric peptides, including the M1145 peptide which show more than 90-fold higher affinity for galanin receptor type 2 over galanin receptor type 1 and a 76-fold higher affinity over galanin receptor type 3. Furthermore, the peptide produces an agonistic effect in vitro seen as an increase in inositol phosphate (IP) accumulation, both in the absence or the presence of galanin. The peptide design with a N-terminal extension of galanin(2-13), prevails new insights in the assembly of novel subtype specific ligands for the galanin receptor family. Preliminary data on peptides further exploring the usage of N-terminal extension shows even higher preferentiality towards the GalR2 and opens new possibilities to clarify the galanin system as a putative drug target.
Place, publisher, year, edition, pages
2009. Vol. 276, 164-164 p.
Biochemistry and Molecular Biology
Research subject Neurochemistry with Molecular Neurobiology
IdentifiersURN: urn:nbn:se:su:diva-45997DOI: 10.1111/j.1742-4658.2009.07049.xOAI: oai:DiVA.org:su-45997DiVA: diva2:370826
34th Congress of the Federation-of-European-Biochemical-Societies, July 04-09, 2009, Prague, Czech Republic
Special Issue: Abstracts of the 34th FEBS Congress2013-01-072010-11-182015-04-21Bibliographically approved