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Important pharmacophores for binding to galanin receptor 2
Stockholm University, Faculty of Science, Department of Neurochemistry and Neurotoxicology.
Stockholm University, Faculty of Science, Department of Neurochemistry and Neurotoxicology.ORCID iD: 0000-0001-6107-0844
2005 (English)In: Neuropeptides, ISSN 0143-4179, E-ISSN 1532-2785, Vol. 39, no 3, 169-171 p.Article in journal (Refereed) Published
Abstract [en]

Galanin(2–11) has been introduced as a receptor subtype selective ligand for the GalR2 subtype of the galanin receptors, and has gained use in pharmacological studies of galaninergic signaling in the past two years. By introducing l-Ala substitutions in the galanin(2–11) sequence, we have examined the amino acid residues which are of importance for binding to the GalR2 receptor. Our study shows that Trp2, Asn5, Gly8 and Tyr9 are of great importance for high affinity binding. When placed in an α-helical conformation, the side chains of these residues are, with the exception of Tyr9, displayed on the same “side” of the peptide. This information is useful in the rational design of non-peptide type GalR2 receptor ligands.

Place, publisher, year, edition, pages
2005. Vol. 39, no 3, 169-171 p.
Keyword [en]
Galanin, Galanin receptors, Galanin(2–11), Galanin receptor selective ligand, L-Ala substitution
National Category
Biological Sciences Chemical Sciences
Identifiers
URN: urn:nbn:se:su:diva-23020OAI: oai:DiVA.org:su-23020DiVA: diva2:189920
Available from: 2007-01-03 Created: 2007-01-03 Last updated: 2017-12-13Bibliographically approved
In thesis
1. Subtype selective activation and molecular characterization of galanin receptors
Open this publication in new window or tab >>Subtype selective activation and molecular characterization of galanin receptors
2007 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

Showing an extensive distribution in the nervous system, and often in co-localization with the classical neurotransmitters, neuropeptides are functioning as important modulators of neuronal signaling. Subsequently, compelling evidence has implicated a modulatory role for the neuropeptide galanin in several physiological functions. The effect of galanin is trancduced intracellularly by three different receptors, and defining the explicit effect from these receptor subtypes is of outmost interest, and likely to result in future therapeutic utilization of the galanin system.

The main aim of this thesis was to improve the development of subtype selective ligands utilized to differentiate between the galanin receptor subtypes. To achieve this, we have designed and developed novel galanin receptor ligands and characterized the molecular interactions necessary for ligand bindig at the GalR2 subtype.

The major findings include the introduction and characterization of two galanin receptor ligands, selectively activating GalR1 or inhibiting GalR2. Although having moderate selectivity, the two ligands have been utilized in a number of studies, pursuing their initial presentation, in order to differentiate between the galanin receptors and to establish their specific function. Further optimization is likely to improve the selectivity and utilization of these ligands. By identifying the major pharmacophores in the Gal(2-11) ligand and the residues in the GalR2 subtype participating in ligand binding, we have been able to characterize the binding site in this receptor subtype and interactions that are of significance for recognition of subtype specific ligands. Together, these findings on GalR2 and Gal(2-11) are of importance for future design of ligands acting on this receptor.

Place, publisher, year, edition, pages
Stockholm: Institutionen för neurokemi, 2007. 87 p.
National Category
Neurosciences
Identifiers
urn:nbn:se:su:diva-1344 (URN)91-7155-325-8 (ISBN)
Public defence
2007-02-02, Magnélisalen, Kemiska övningslaboratoriet, Svante Arrhenius väg 12 A, Stockholm, 13:00 (English)
Opponent
Supervisors
Available from: 2007-01-03 Created: 2007-01-03 Last updated: 2010-02-24Bibliographically approved

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