The quest for a GPCR subtype selective ligand for the galanin system: development and utilization
2012 (English)Conference paper (Other academic)
The family of GPCR’s has for long served as the most common pharmaceutical drug target. Even so, some receptors have failed to show potent interactions when exposed to big screenings libraries in the past. Three of these receptors are the so called galanin receptors (GalR).
Galanin is a neuroendocrine peptide that is widely distributed in both the CNS and PNS, as well as in the endocrine system. Galanin has been shown to influence several physiological processes including cognition, affective behavior, nerve injury, Alzheimer’s disease, neuroregeneration, seizures, feeding, and hormone release. The regionally specific expression of the galanin receptors (GalR1-3) suggests different physiological roles, a feature which mostly remains unexplored due to the lack of selective ligands acting on the GalR subtypes. The galanin research field has until very recently been struggling with the limitation of having neither receptor subtype specific ligands nor antibodies. Recently, we and others have successfully developed pharmacological tools for the galanin research field, including allosteric modulators, BBB-penetrating ligands and receptor subtype specific ligand.
We here present several promising ligands that are GalR subtype selective [Runesson 2009, Saar 2011, several manuscripts in preparations] and these might be future candidates to unravel the function of GalR subtypes. The goal of this poster will be to present our latest tools and some results from animal studies with models related to depression, seizures and feeding. We find these new developments of pivotal interest for the galanin research field and hope that this neuropeptide will now be revived and that new and old findings could be translated into the clinical setting.
Place, publisher, year, edition, pages
GPCR, Receptor, Neuropeptide, Galanin, Receptor ligand
Neurosciences Biochemistry and Molecular Biology
Research subject Neurochemistry with Molecular Neurobiology
IdentifiersURN: urn:nbn:se:su:diva-75091OAI: oai:DiVA.org:su-75091DiVA: diva2:514072
8th FENS Forum of Neuroscience. July 14 2012 -