Orthosteric,Allosteric and Biased Signalling at the Relaxin-3 Receptor RXFP3 |
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Authors: | Martina Kocan Sheng Yu Ang Roger J Summers |
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Institution: | 1.Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences,Monash University,Melbourne,Australia |
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Abstract: | Relaxin-3 is a neuropeptide that has roles in stress, memory and appetite regulation. The peptide acts on its cognate receptor RXFP3 to induce coupling to inhibitory G proteins to inhibit adenylyl cyclase and activate MAP-kinases such as ERK1/2, p38MAPK and JNK. Other relaxin family peptides can activate the receptor to produce alternative patterns of signalling and there is an allosteric modulator 135PAM1 that displays probe-selectivity. There are now a variety of selective peptide agonists and antagonists that will assist in the determination of the physiological roles of the relaxin-RXFP3 system and its potential as a drug target. |
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