Related Experiment Video
Updated: Aug 17, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Important pharmacophores for binding to galanin receptor 2
Linda Lundström1, Xiaoying Lu, Ulo Langel
1Department of Neurochemistry and Neurotoxicology, Stockholm University, Svante Arrheniusv. 21A, 106 91 Stockholm, Sweden. lindal@neurochem.su.se
Abstract:
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 alpha-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.
Related Concept Videos
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G-protein Coupled Receptors
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...

