Orthosteric, allosteric and biased signalling at the relaxin-3 receptor RXFP3

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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.
Original languageEnglish
Pages (from-to)610-619
Number of pages10
JournalNeurochemical Research
Issue number3
Publication statusPublished - 2016


  • Allosteric modulator
  • Biased signalling
  • Relaxin-3
  • RXFP3

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