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Compound class:
Peptide or derivative
Comment: GRASP is a 29-amino acid peptide that acts as an agonist at the GDF15 receptor GFRAL/RET [1]. It binds to the GFRAL extracellular domain at a site distinct from the GDF15 binding site. GRASP was designed to explore the potential of disrupting GFRAL signaling as a mechanism to attenuate GDF15- and chemotherapy-induced nausea and cachexia.
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 |
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1. Borner T, Tinsley IC, Milliken BT, Doebley SA, Najjar NR, Kerwood DJ, De Jonghe BC, Hayes MR, Doyle RP. (2023)
Creation of a Peptide Antagonist of the GFRAL-RET Receptor Complex for the Treatment of GDF15-Induced Malaise. J Med Chem, 66 (16): 11237-11249. [PMID:37506293] |
