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- Runesson, Johan, 1980-, et al.
(författare)
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A novel GalR2-specific peptide agonist
- 2009
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Ingår i: Neuropeptides. - : Elsevier BV. - 0143-4179 .- 1532-2785. ; 43:3, s. 187-192
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Tidskriftsartikel (refereegranskat)abstract
- The galanin peptide family and its three receptors have with compelling evidence been implicated in several high-order physiological disorders. The co-localization with other neuromodulators and the distinct up-regulation during and after pathological disturbances has drawn attention to this neuropeptide family. In the current study we present data on receptor binding and functional response for a novel galanin receptor type 2 (GalR2) selective chimeric peptide, M1145 [(RG)(2)-N-galanin(2-13)-VL-(P)(3)-(AL)(2)-A-amide]. The M1145 peptide shows more than 90-fold higher affinity for GalR2 over GalR1 and a 76-fold higher affinity over GalR3. Furthermore, the peptide yields 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 and opens new possibilities to apply the galanin system as a putative drug target.
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| 4. |
- Runesson, Johan, 1980-, et al.
(författare)
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Novel peptide agonists, favoring galanin receptor type 2 over galanin receptor type 1 and 3
- 2009
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Ingår i: The FEBS Journal. - : Wiley. - 1742-464X .- 1742-4658. ; 276, s. 164-164
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Tidskriftsartikel (refereegranskat)abstract
- 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.
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