Synonyms: insulin-like peptide 5
Compound class:
Endogenous peptide in human, mouse or rat
Species: Human
Ligand Activity Visualisation ChartsThese 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. ✖ |
References |
1. Ang SY, Evans BA, Poole DP, Bron R, DiCello JJ, Bathgate RAD, Kocan M, Hutchinson DS, Summers RJ. (2018)
INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells. J Mol Endocrinol, 60 (3): 213-224. [PMID:29535183] |
2. Ang SY, Hutchinson DS, Patil N, Evans BA, Bathgate RAD, Halls ML, Hossain MA, Summers RJ, Kocan M. (2017)
Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor. Br J Pharmacol, 174 (10): 1077-1089. [PMID:27243554] |
3. Belgi A, Bathgate RA, Kocan M, Patil N, Zhang S, Tregear GW, Wade JD, Hossain MA. (2013)
Minimum active structure of insulin-like peptide 5. J Med Chem, 56 (23): 9509-16. [PMID:24188028] |
4. Khalaf MS, Coles MP, Hitchcock PB. (2008)
A structural, theoretical and coordinative evaluation of the bicyclic guanidinate derived from 1,4,6-triazabicyclo[3.3.0]oct-4-ene. Dalton Trans, (32): 4288-95. [PMID:18682868] |
5. 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] |
6. 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] |
7. Liu C, Kuei C, Sutton S, Chen J, Bonaventure P, Wu J, Nepomuceno D, Kamme F, Tran DT, Zhu J et al.. (2005)
INSL5 is a high affinity specific agonist for GPCR142 (GPR100). J Biol Chem, 280 (1): 292-300. [PMID:15525639] |
8. Patil NA, Bathgate RAD, Kocan M, Ang SY, Tailhades J, Separovic F, Summers R, Grosse J, Hughes RA, Wade JD et al.. (2016)
The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity. Amino Acids, 48 (4): 987-992. [PMID:26661035] |
9. Patil NA, Hughes RA, Rosengren KJ, Kocan M, Ang SY, Tailhades J, Separovic F, Summers RJ, Grosse J, Wade JD et al.. (2016)
Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist. J Med Chem, 59 (5): 2118-25. [PMID:26824523] |
10. 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] |
11. 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] |
12. Wang XY, Guo YQ, Shao XX, Liu YL, Xu ZG, Guo ZY. (2014)
Identification of important residues of insulin-like peptide 5 and its receptor RXFP4 for ligand-receptor interactions. Arch Biochem Biophys, 558: 127-32. [PMID:25043977] |
13. 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] |