Abstract
| Original language | English |
|---|---|
| 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
Cite this
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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 journal › Article › Research › peer-review
TY - JOUR
T1 - Orthosteric, allosteric and biased signalling at the relaxin-3 receptor RXFP3
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
UR - http://link.springer.com.ezproxy.lib.monash.edu.au/content/pdf/10.1007%2Fs11064-015-1701-3.pdf
U2 - 10.1007/s11064-015-1701-3
DO - 10.1007/s11064-015-1701-3
M3 - Article
VL - 41
SP - 610
EP - 619
JO - Neurochemical Research
JF - Neurochemical Research
SN - 0364-3190
IS - 3
ER -