title: Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3.
abstract: Relaxin-3 and its endogenous receptor RXFP3 are involved in fundamental neurological signalling pathways, such as learning and memory, stress, feeding and addictive behaviour. Consequently, this signalling system has emerged as an attractive drug target. Development of leads targeting RXFP3 relies on assays for screening and ligand optimization. Here, we present the synthesis and in vitro characterization of a fluorescent europium-labelled antagonist of RXFP3. This ligand represents a cheap and safe but powerful tool for future mechanistic and cell-based receptor-ligand interaction studies of the RXFP3 receptor.
authors: The University of Queensland, School of Biomedical Sciences, St Lucia, Brisbane, QLD, 4072, Australia.
authors: Linda M
authors: LM
authors: Haugaard-Kedström
authors: Lilian L L
authors: LL
authors: Wong
authors: Ross A D
authors: RA
authors: Bathgate
authors: K Johan
authors: KJ
authors: Rosengren
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D005063:Europium / Q000737:chemistry / Q000494:pharmacology; D006574:Heterocyclic Compounds, 2-Ring / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D012065:Relaxin / Q000737:chemistry
chemical_list: D006574:Heterocyclic Compounds, 2-Ring; C480238:RLN3 protein, human; C410092:RXFP3 protein, human; D043562:Receptors, G-Protein-Coupled; D005063:Europium; D012065:Relaxin