title: Orthosteric, Allosteric and Biased Signalling at the Relaxin-3 Receptor RXFP3.
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.
authors: Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, 399 Royal Parade, Parkville, Melbourne, VIC, 3052, Australia.
authors: Martina
authors: M
authors: Kocan
authors: Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, 399 Royal Parade, Parkville, Melbourne, VIC, 3052, Australia.
authors: Sheng Yu
authors: SY
authors: Ang
authors: Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, 399 Royal Parade, Parkville, Melbourne, VIC, 3052, Australia. Roger.Summers@monash.edu.
authors: Roger J
authors: RJ
authors: Summers
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D019390:Arrestins / Q000378:metabolism; D066246:ErbB Receptors / Q000235:genetics / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D018000:Receptors, Peptide / Q000378:metabolism*; D012065:Relaxin / Q000378:metabolism; D015398:Signal Transduction; D015533:Transcriptional Activation; D000071557:beta-Arrestins
chemical_list: D019390:Arrestins; C410092:RXFP3 protein, human; C577472:RXFP3 protein, rat; D043562:Receptors, G-Protein-Coupled; D018000:Receptors, Peptide; C505050:SALPR protein, mouse; D000071557:beta-Arrestins; D012065:Relaxin; D066246:ErbB Receptors; D019204:GTP-Binding Proteins
keywords: Allosteric modulator; Biased signalling; RXFP3; Relaxin-3