Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3

Amino Acids
Linda M Haugaard-KedströmK Johan Rosengren

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.

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Citations

Aug 9, 2016·Peptides·Tharindunee JayakodyGavin Stewart Dawe
Aug 23, 2018·The Journal of Biological Chemistry·Lilian L L WongRoss A D Bathgate
Aug 23, 2018·The Journal of Biological Chemistry·Linda M Haugaard-KedströmK Johan Rosengren
Jun 21, 2019·British Journal of Pharmacology·Subhi MarwariGavin Stewart Dawe
Nov 30, 2019·Scientific Reports·Praveen PraveenMohammed Akhter Hossain
Mar 7, 2020·Frontiers in Chemistry·Han Siean LeeK Johan Rosengren

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