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Synonyms: P2pal-18S
Compound class:
Peptide or derivative
Comment: Pepducins are membrane tethered mimics of intracellular loops of the target receptor. They are designed to interact with regions of the target receptor identified as being involved in signal transduction. Pepducins are able to modify receptor activity by flipping across the lipid membrane and where they are able to interact with the targeted portions of the native receptor. P2pal18S is an intracellualr loop 3 pepducin that acts as an antagonist at the PAR2 receptor [1].
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. ✖ |
Peptide Sequence  |
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| RSSAMDENSEKKRKSAIK | |
| Arg-Ser-Ser-Ala-Met-Asp-Glu-Asn-Ser-Glu-Lys-Lys-Arg-Lys-Ser-Ala-Ile-Lys | |
| Chemical Modification | |
| The peptide is N-palmitoylated (C13H31CONH) and amidated on the C terminal. This creates a 'pepducin', a membrane tethered mimic of the third intracellular loop of PAR2, with amino acid substitution R284S (position 15 of the synthetic peptide). | |
