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Compound class:
Peptide or derivative
Comment: This peptide is a mesotrypsin (PRSS3) inhibitor based upon the BPTI (bovine pancreatic trypsin inhibitor aka aprotinin) scaffold with P1 (Lys15 to Arg) and P2′ (Arg17 to Gly) modifications [1]. PRSS3 is an atypical isoform of trypsin. Its up-regulation may promote tumour progression. Hence, PRSS3 inhibitors are being investigated as anti-cancer agents.
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. Salameh MA, Soares AS, Hockla A, Radisky DC, Radisky ES. (2011)
The P(2)' residue is a key determinant of mesotrypsin specificity: engineering a high-affinity inhibitor with anticancer activity. Biochem J, 440 (1): 95-105. [PMID:21806544] |
