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

Research output: Contribution to journalArticleResearchpeer-review

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.
Original languageEnglish
Pages (from-to)610-619
Number of pages10
JournalNeurochemical Research
Volume41
Issue number3
DOIs
Publication statusPublished - 2016

Keywords

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

Cite this

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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.",
keywords = "Allosteric modulator, Biased signalling, Relaxin-3, RXFP3",
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Orthosteric, allosteric and biased signalling at the relaxin-3 receptor RXFP3. / Kocan, Martina; Ang, Sheng Yu; Summers, Roger J.

In: Neurochemical Research, Vol. 41, No. 3, 2016, p. 610-619.

Research output: Contribution to journalArticleResearchpeer-review

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