BPTI-K15R/R17G   Click here for help

GtoPdb Ligand ID: 7897

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.
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Selectivity at enzymes
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
serine protease 3 Hs Inhibitor Inhibition 8.2 pKi - 1
pKi 8.2 (Ki 5.9x10-9 M) [1]