relaxin-3   Click here for help

GtoPdb Ligand ID: 1990

Synonyms: H3 relaxin
Compound class: Endogenous peptide in human, mouse or rat
Comment: A heterodimer containing disulfide-linked A and B subunits that are each cleaved from the relaxin 3 gene (RLN3) product.
Species: Human
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Ang SY, Hutchinson DS, Evans BA, Hossain MA, Patil N, Bathgate RA, Kocan M, Summers RJ. (2017)
The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.
Naunyn Schmiedebergs Arch Pharmacol, 390 (1): 105-111. [PMID:27888281]
2. Bathgate RA, Lin F, Hanson NF, Otvos L, Guidolin A, Giannakis C, Bastiras S, Layfield SL, Ferraro T, Ma S, Zhao C, Gundlach AL, Samuel CS, Tregear GW, Wade JD. (2006)
Relaxin-3: Improved Synthesis Strategy and Demonstration of Its High-Affinity Interaction with the Relaxin Receptor LGR7 Both In Vitro and In Vivo.
Biochemistry, 45: 1043-1053. [PMID:16411781]
3. Chen J, Kuei C, Sutton SW, Bonaventure P, Nepomuceno D, Eriste E, Sillard R, Lovenberg TW, Liu C. (2005)
Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species.
J Pharmacol Exp Ther, 312 (1): 83-95. [PMID:15367576]
4. Halls ML, Bond CP, Sudo S, Kumagai J, Ferraro T, Layfield S, Bathgate RA, Summers RJ. (2005)
Multiple binding sites revealed by interaction of relaxin family peptides with native and chimeric relaxin family peptide receptors 1 and 2 (LGR7 and LGR8).
J Pharmacol Exp Ther, 313 (2): 677-87. [PMID:15649866]
5. Hossain MA, Rosengren KJ, Haugaard-Jönsson LM, Zhang S, Layfield S, Ferraro T, Daly NL, Tregear GW, Wade JD, Bathgate RA. (2008)
The A-chain of human relaxin family peptides has distinct roles in the binding and activation of the different relaxin family peptide receptors.
J Biol Chem, 283 (25): 17287-97. [PMID:18434306]
6. Kocan M, Sarwar M, Hossain MA, Wade JD, Summers RJ. (2014)
Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).
Br J Pharmacol, 171 (11): 2827-41. [PMID:24641548]
7. Kuei C, Sutton S, Bonaventure P, Pudiak C, Shelton J, Zhu J, Nepomuceno D, Wu J, Chen J, Kamme F et al.. (2007)
R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization.
J Biol Chem, 282 (35): 25425-35. [PMID:17606621]
8. Kumagai J, Hsu SY, Matsumi H, Roh JS, Fu P, Wade JD, Bathgate RA, Hsueh AJ. (2002)
INSL3/Leydig insulin-like peptide activates the LGR8 receptor important in testis descent.
J Biol Chem, 277 (35): 31283-6. [PMID:12114498]
9. Liu C, Chen J, Kuei C, Sutton S, Nepomuceno D, Bonaventure P, Lovenberg TW. (2005)
Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7.
Mol Pharmacol, 67 (1): 231-40. [PMID:15465925]
10. Liu C, Chen J, Sutton S, Roland B, Kuei C, Farmer N, Sillard R, Lovenberg TW. (2003)
Identification of relaxin-3/INSL7 as a ligand for GPCR142.
J Biol Chem, 278 (50): 50765-70. [PMID:14522967]
11. Liu C, Eriste E, Sutton S, Chen J, Roland B, Kuei C, Farmer N, Jörnvall H, Sillard R, Lovenberg TW. (2003)
Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.
J Biol Chem, 278 (50): 50754-64. [PMID:14522968]
12. Praveen P, Bathgate RAD, Hossain MA. (2019)
Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Sci Rep, 9 (1): 17828. [PMID:31780677]
13. Shabanpoor F, Akhter Hossain M, Ryan PJ, Belgi A, Layfield S, Kocan M, Zhang S, Samuel CS, Gundlach AL, Bathgate RA et al.. (2012)
Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
J Med Chem, 55 (4): 1671-81. [PMID:22257012]
14. Sudo S, Kumagai J, Nishi S, Layfield S, Ferraro T, Bathgate RA, Hsueh AJ. (2003)
H3 relaxin is a specific ligand for LGR7 and activates the receptor by interacting with both the ectodomain and the exoloop 2.
J Biol Chem, 278 (10): 7855-62. [PMID:12506116]
15. van der Westhuizen ET, Christopoulos A, Sexton PM, Wade JD, Summers RJ. (2010)
H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).
Mol Pharmacol, 77 (5): 759-72. [PMID:20159943]
16. van der Westhuizen ET, Werry TD, Sexton PM, Summers RJ. (2007)
The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.
Mol Pharmacol, 71 (6): 1618-29. [PMID:17351017]
17. Zhu J, Kuei C, Sutton S, Kamme F, Yu J, Bonaventure P, Atack J, Lovenberg TW, Liu C. (2008)
Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135).
Eur J Pharmacol, 590 (1-3): 43-52. [PMID:18582868]