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

Haugaard-Kedstrom, Linda M, Wong, Lillian L. L, Bathgate, Ross A. D and Rosengren, K. Johan (2015) Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3. Amino Acids, 47 6: 1267-1271. doi:10.1007/s00726-015-1961-x


Author Haugaard-Kedstrom, Linda M
Wong, Lillian L. L
Bathgate, Ross A. D
Rosengren, K. Johan
Title Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3
Journal name Amino Acids   Check publisher's open access policy
ISSN 1438-2199
0939-4451
Publication date 2015-06-01
Year available 2015
Sub-type Article (original research)
DOI 10.1007/s00726-015-1961-x
Open Access Status
Volume 47
Issue 6
Start page 1267
End page 1271
Total pages 5
Place of publication Wien, Austria
Publisher Springer Wien
Language eng
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.
Keyword R3B1-22R
Europium
Relaxin family peptide receptor-3 (RXFP3)
Relaxin-3
Q-Index Code C1
Q-Index Status Confirmed Code
Grant ID APP1066369
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
School of Biomedical Sciences Publications
 
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