Projects per year
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 language | English |
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Pages (from-to) | 610-619 |
Number of pages | 10 |
Journal | Neurochemical Research |
Volume | 41 |
Issue number | 3 |
DOIs | |
Publication status | Published - 2016 |
Keywords
- Allosteric modulator
- Biased signalling
- Relaxin-3
- RXFP3
Projects
- 1 Finished
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The Janus face of G Protein-Coupled Receptors: Implications for Disease Mechanisms and Opportunities for Drug Discovery
Sexton, P. (Primary Chief Investigator (PCI)), Bunnett, N. (Chief Investigator (CI)), Christopoulos, A. (Chief Investigator (CI)) & Summers, R. (Chief Investigator (CI))
National Health and Medical Research Council (NHMRC) (Australia)
1/01/14 → 31/12/18
Project: Research