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Literature summary for 3.4.21.109 extracted from

  • Quimbar, P.; Malik, U.; Sommerhoff, C.P.; Kaas, Q.; Chan, L.Y.; Huang, Y.H.; Grundhuber, M.; Dunse, K.; Craik, D.J.; Anderson, M.A.; Daly, N.L.
    High-affinity cyclic peptide matriptase inhibitors (2013), J. Biol. Chem., 288, 13885-13896.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
ARCTKSIPPICFPD a mutant of sunflower trypsin inhibitor-18 Homo sapiens
GACTKSIPPICFPD a mutant of sunflower trypsin inhibitor-17 Homo sapiens
GAVCPKILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGACPKILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGRCPKALKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGRCPKILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCAKILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPAILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKALKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKIAKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILAKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILKACRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILKKCRRDSDCPGACICRGAGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILKKCRRDSDCPGACICRGNGACGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILKKCRRDSDCPGACICRGNGYCASGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKILKKCRRDSDCPGACICRGNGYCGAGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPKRLKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GGVCPRILKKCRRDSDCPGACICRGNGYCGSGSD a mutant of Momordica cochinchinensis trypsin inhibitor-II Homo sapiens
GKCTKSIPPICFPD a mutant of sunflower trypsin inhibitor-6 Homo sapiens
GRCAKSIPPICFPD a mutant of sunflower trypsin inhibitor-16 Homo sapiens
GRCTASIPPICFPD a mutant of sunflower trypsin inhibitor-15 Homo sapiens
GRCTKAIPPICFPD a mutant of sunflower trypsin inhibitor-14 Homo sapiens
GRCTKSAPPICFPD a mutant of sunflower trypsin inhibitor-13 Homo sapiens
GRCTKSAPPRCFPD a mutant of sunflower trypsin inhibitor-1 Homo sapiens
GRCTKSIAPICFPD a mutant of sunflower trypsin inhibitor-12 Homo sapiens
GRCTKSIPAICFPD a mutant of sunflower trypsin inhibitor-11 Homo sapiens
GRCTKSIPPACFPD a mutant of sunflower trypsin inhibitor-10 Homo sapiens
GRCTKSIPPDCFPD a mutant of sunflower trypsin inhibitor-3 Homo sapiens
GRCTKSIPPGCFPD a mutant of sunflower trypsin inhibitor-2 Homo sapiens
GRCTKSIPPICAPD a mutant of sunflower trypsin inhibitor-9 Homo sapiens
GRCTKSIPPICFAD a mutant of sunflower trypsin inhibitor-8 Homo sapiens
GRCTKSIPPICFPA a mutant of sunflower trypsin inhibitor-7 Homo sapiens
GRCTKSIPPICFPD
-
Homo sapiens
GRCTKSIPPKCFPD a mutant of sunflower trypsin inhibitor-0 Homo sapiens
GRCTKSIPPRCFPD a mutant of sunflower trypsin inhibitor-1 Homo sapiens
GRCTKSRPPICFPD a mutant of sunflower trypsin inhibitor-4 Homo sapiens
GRCTRSIPPICFPD a mutant of sunflower trypsin inhibitor-5 Homo sapiens
additional information synthesis of high-affinity cyclic peptide matriptase inhibitors. An analogue of Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) is one of the most potent inhibitors of matriptase, structure-activity relationships of SFTI-1 and MCoTI-II, which is a structurally divergent trypsin inhibitor also containing a cyclic backbone Homo sapiens
sunflower trypsin inhibitor-1 SFTI-1, GRCTKSIPPICFPD, the plant-derived cyclic peptide is a promising drug scaffold with potent matriptase inhibitory activity, three-dimensional structure of the inhibitor and the protease domain of matriptase, molecular modeling, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane type II transmembrane serine protease matriptase Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5Y6
-
-

Source Tissue

Source Tissue Comment Organism Textmining
epithelium high expression level in epithelia Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzoyl-L-arginine-4-methylcoumaryl-7-amide + H2O
-
Homo sapiens benzoyl-L-arginine + 7-amino-4-methylcoumarin
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000029
-
GGRCPKILKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.0000023
-
GGACPKILKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.0000035
-
GGRCPKALKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.0000037
-
GGVCPKILKKCRRDSDCPGACICRGNGYCASGSD pH 7,6, 37°C Homo sapiens
0.0000041
-
GGVCPKILKACRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.0000064
-
GRCTKSIPPRCFPD pH 7,6, 37°C Homo sapiens
0.0000098
-
GGVCPKALKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.000011
-
GGVCPKILKKCRRDSDCPGACICRGNGACGSGSD pH 7,6, 37°C Homo sapiens
0.000012
-
GGVCPKIAKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.000012
-
GGVCPKILKKCRRDSDCPGACICRGAGYCGSGSD pH 7,6, 37°C Homo sapiens
0.000027
-
GRCTKSIAPICFPD pH 7,6, 37°C Homo sapiens
0.000039
-
GGVCAKILKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.000039
-
GGVCPRILKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.00004
-
GRCTKSIPPKCFPD pH 7,6, 37°C Homo sapiens
0.000051
-
GRCTKSAPPRCFPD pH 7,6, 37°C Homo sapiens
0.000073
-
GRCTKSIPPACFPD pH 7,6, 37°C Homo sapiens
0.000076
-
GGVCPKILAKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.000084
-
GRCTKSAPPICFPD pH 7,6, 37°C Homo sapiens
0.000098
-
GGVCPKILKKCRRDSDCPGACICRGNGYCGAGSD pH 7,6, 37°C Homo sapiens
0.00011
-
GGVCPKRLKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.00018
-
GAVCPKILKKCRRDSDCPGACICRGNGYCGSGSD pH 7,6, 37°C Homo sapiens
0.00019
-
ARCTKSIPPICFPD pH 7,6, 37°C Homo sapiens
0.0002
-
GRCTKSIPPICFPD pH 7,6, 37°C Homo sapiens
0.00024
-
GRCTKSIPPICFAD pH 7,6, 37°C Homo sapiens
0.00031
-
GRCTRSIPPICFPD pH 7,6, 37°C Homo sapiens
0.00032
-
GRCTKSIPPICAPD pH 7,6, 37°C Homo sapiens
0.00037
-
GRCTKSIPAICFPD pH 7,6, 37°C Homo sapiens
0.0012
-
GKCTKSIPPICFPD pH 7,6, 37°C Homo sapiens
0.0015
-
GRCAKSIPPICFPD pH 7,6, 37°C Homo sapiens
0.0015
-
GRCTKSIPPICFPA pH 7,6, 37°C Homo sapiens
0.0016
-
GRCTKAIPPICFPD pH 7,6, 37°C Homo sapiens
0.0037
-
GRCTKSIPPGCFPD pH 7,6, 37°C Homo sapiens
0.0045
-
GRCTKSRPPICFPD pH 7,6, 37°C Homo sapiens
0.01
-
GRCTASIPPICFPD above, pH 7,6, 37°C Homo sapiens
0.01
-
GGVCPAILKKCRRDSDCPGACICRGNGYCGSGSD above, pH 7,6, 37°C Homo sapiens
0.01
-
GACTKSIPPICFPD pH 7,6, 37°C Homo sapiens
0.01
-
GRCTKSIPPDCFPD pH 7,6, 37°C Homo sapiens

General Information

General Information Comment Organism
additional information comparison of trypsin and matriptase active sites, overview Homo sapiens
physiological function the type II transmembrane serine protease matriptase is a key activator of multiple signaling pathways associated with cell proliferation and modification of the extracellular matrix Homo sapiens