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Compound class: Endogenous peptide in human, mouse or rat
Comment: There is some ambiguity in the literature and on other resources as to the exact chemical structure and stereochemistry of ghrelin. In the absence of a consensus chemical structure, we have chosen not to include an image of the molecule on this ligand entry. However, for representations of the structure please see these CHEBI:75431, CHEMBL425281 and PubChem CID 16133832 entries.
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.✖
View more information in the IUPHAR Pharmacology Education Project: ghrelin
1. Bedendi I, Alloatti G, Marcantoni A, Malan D, Catapano F, Ghé C, Deghenghi R, Ghigo E, Muccioli G. (2003)
Cardiac effects of ghrelin and its endogenous derivatives des-octanoyl ghrelin and des-Gln14-ghrelin.
Eur J Pharmacol, 476 (1-2): 87-95. [PMID:12969753]
2. Ge X, Yang H, Bednarek MA, Galon-Tilleman H, Chen P, Chen M, Lichtman JS, Wang Y, Dalmas O, Yin Y et al.. (2018)
LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor.
Cell Metab, 27 (2): 461-469.e6. [PMID:29233536]
3. Holst B, Brandt E, Bach A, Heding A, Schwartz TW. (2005)
Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling.
Mol Endocrinol, 19 (9): 2400-11. [PMID:15905359]
4. Holst B, Cygankiewicz A, Jensen TH, Ankersen M, Schwartz TW. (2003)
High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.
Mol Endocrinol, 17 (11): 2201-10. [PMID:12907757]
5. Matsumoto M, Hosoda H, Kitajima Y, Morozumi N, Minamitake Y, Tanaka S, Matsuo H, Kojima M, Hayashi Y, Kangawa K. (2001)
Structure-activity relationship of ghrelin: pharmacological study of ghrelin peptides.
Biochem Biophys Res Commun, 287 (1): 142-6. [PMID:11549267]
6. Muccioli G, Papotti M, Locatelli V, Ghigo E, Deghenghi R. (2001)
Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland.
J Endocrinol Invest, 24 (3): RC7-9. [PMID:11314756]
7. Palyha OC, Feighner SD, Tan CP, McKee KK, Hreniuk DL, Gao YD, Schleim KD, Yang L, Morriello GJ, Nargund R et al.. (2000)
Ligand activation domain of human orphan growth hormone (GH) secretagogue receptor (GHS-R) conserved from Pufferfish to humans.
Mol Endocrinol, 14 (1): 160-9. [PMID:10628755]
8. Sivertsen B, Lang M, Frimurer TM, Holliday ND, Bach A, Els S, Engelstoft MS, Petersen PS, Madsen AN, Schwartz TW et al.. (2011)
Unique interaction pattern for a functionally biased ghrelin receptor agonist.
J Biol Chem, 286 (23): 20845-60. [PMID:21402696]