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

Martina Kocan; Sheng Yu Ang; Roger J Summers

doi:10.1007/s11064-015-1701-3

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

Martina Kocan, Sheng Yu Ang, Roger J Summers

Research output: Contribution to journal › Article › Research › peer-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 language	English
Pages (from-to)	610-619
Number of pages	10
Journal	Neurochemical Research
Volume	41
Issue number	3
DOIs	https://doi.org/10.1007/s11064-015-1701-3
Publication status	Published - 2016

Keywords

Allosteric modulator
Biased signalling
Relaxin-3
RXFP3

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10.1007/s11064-015-1701-3

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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. ",

keywords = "Allosteric modulator, Biased signalling, Relaxin-3, RXFP3",

author = "Martina Kocan and Ang, {Sheng Yu} and Summers, {Roger J}",

year = "2016",

doi = "10.1007/s11064-015-1701-3",

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journal = "Neurochemical Research",

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AU - Kocan, Martina

AU - Ang, Sheng Yu

AU - Summers, Roger J

PY - 2016

Y1 - 2016

N2 - 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.

AB - 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.

KW - Allosteric modulator

KW - Biased signalling

KW - Relaxin-3

KW - RXFP3

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M3 - Article

SN - 0364-3190

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SP - 610

EP - 619

JO - Neurochemical Research

JF - Neurochemical Research

IS - 3

ER -

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

Abstract

Keywords

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The Janus face of G Protein-Coupled Receptors: Implications for Disease Mechanisms and Opportunities for Drug Discovery

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

Abstract

Keywords

Access to Document

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The Janus face of G Protein-Coupled Receptors: Implications for Disease Mechanisms and Opportunities for Drug Discovery

Cite this