Haugaard-Kedström Linda M, Wong Lilian L L, Bathgate Ross A D, Rosengren K Johan
The University of Queensland, School of Biomedical Sciences, St Lucia, Brisbane, QLD, 4072, Australia.
Amino Acids. 2015 Jun;47(6):1267-71. doi: 10.1007/s00726-015-1961-x. Epub 2015 Mar 20.
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.
松弛素-3及其内源性受体RXFP3参与了诸如学习与记忆、应激、进食和成瘾行为等基本神经信号通路。因此，该信号系统已成为一个有吸引力的药物靶点。靶向RXFP3的先导化合物的开发依赖于筛选和配体优化的检测方法。在此，我们展示了一种铕标记的RXFP3荧光拮抗剂的合成及其体外特性。这种配体是一种廉价、安全但功能强大的工具，可用于未来对RXFP3受体进行基于机制和细胞的受体-配体相互作用研究。
