3.4.21.109: matriptase
This is an abbreviated version!
For detailed information about matriptase, go to the full flat file.
Word Map on EC 3.4.21.109
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3.4.21.109
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hepatocyte
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hepcidin
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hai-1
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anemia
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metastasis
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prostate
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hepsin
-
zymogen
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transferrin
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prostasin
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overload
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trypsin-like
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irida
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plasminogen
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hemojuvelin
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iron-refractory
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kunitz-type
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inhibitor-1
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kunitz
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ttsps
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hemochromatosis
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erythropoiesis
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microcytic
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membrane-anchored
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urokinase-type
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ferroportin
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iron-deficiency
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pro-hgf
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pericellular
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upa
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autoactivation
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two-chain
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hypochromic
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medicine
-
protease-activated
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tmprss4
-
spint2
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corpuscular
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erythroferrone
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profilaggrin
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camostat
-
corin
-
epithelial-derived
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par-2
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hypotrichosis
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drug development
-
diagnostics
- 3.4.21.109
- hepatocyte
- hepcidin
- hai-1
- anemia
- metastasis
- prostate
- hepsin
- zymogen
- transferrin
- prostasin
- overload
-
trypsin-like
-
irida
- plasminogen
- hemojuvelin
-
iron-refractory
-
kunitz-type
- inhibitor-1
-
kunitz
-
ttsps
- hemochromatosis
-
erythropoiesis
-
microcytic
-
membrane-anchored
-
urokinase-type
-
ferroportin
-
iron-deficiency
- pro-hgf
-
pericellular
- upa
-
autoactivation
-
two-chain
-
hypochromic
- medicine
-
protease-activated
-
tmprss4
-
spint2
-
corpuscular
-
erythroferrone
- profilaggrin
- camostat
- corin
-
epithelial-derived
- par-2
- hypotrichosis
- drug development
- diagnostics
Reaction
cleaves various synthetic substrates with Arg or Lys at the P1 position and prefers small side-chain amino acids, such as Ala and Gly, at the P2 position =
Synonyms
Epi/MTP, epithin, epithin/matriptase, influenza virus-activating protease, matriptase, matriptase-1, matriptase-2, matriptase-3, matriptase1, matriptase1a, membrane-type serine protease 1, membrane-type serine protease 1/matripase, membrane-type serine protease-1, membrane-type serine protease1, membrane-type serine proteinase matripase, membrane-type serine proteinase matriptase, More, MT-2, MT-SP-1, MT-SP1, MT-SP1/matripase, MT2, notopleural, prostamin, PRSS14, r-matripase, serine protease matriptase-2, serine protease SNC19/matripase, SNC19, ST-14, ST14, suppression of tumorigenecity 14, suppressor of tumorigenicity 14, suppressor of tumorigenicity 14 protein, suppressor of tumorigenicity-14, TADG-15, TADG15, TMPRSS6, transmembrane serine protease 6, tumor-associated differentially expressed gene-15, tumor-associated type II transmembrane serine protease, type 2 transmembrane serine protease, type II transmembrane protease, type II transmembrane serine protease
ECTree
3.4.21.109 matriptaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.21.109 - matriptase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(1r,4r)-4-amino-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)cyclohexanecarboxamide
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(2R)-1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-2-carboxylic acid
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(2S)-1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-2-carboxylic acid
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1-(2-aminoethyl)-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)piperidine-4-carboxamide
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1-(3-aminopropanoyl)-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)piperidine-4-carboxamide
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1-(N-[[3-(b-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-3-carboxamide
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1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-4-carboxamide
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3,5-bis(4-carbamimidoylphenoxy)-N-((4-hydroxycyclohexyl)methyl)benzamide
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3,5-bis(4-carbamimidoylphenoxy)-N-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide
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3-(3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl)benzenecarboximidamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
3-[(2R)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2R)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]propyl]benzenecarboximidamide
-
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3-[(2S)-2-([[3-(4-aminobutyl)phenyl]sulfonyl]amino)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-2-[[(2',4'-dimethoxybiphenyl-3-yl)sulfonyl]amino]-3-(4-[2-(methylcarbamoyl)aminoethyl]piperidin-1-yl)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(1H-indol-5-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(2-methylpyrimidin-4-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-aminopyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[4'-(1-methylethoxy)biphenyl-3-yl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(biphenyl-3-ylsulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropoxy]benzenecarboximidamide
higher cytotoxic effect, enzyme-bound structure, crystal structure analysis, overview
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[([3-[(3-aminopropyl)amino]phenyl]sulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(2',4'-dichlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(2'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3',4'-dimethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(3'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-chlorobiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-methoxybiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4-cyclohexylphenyl)sulfonyl]amino]-3-oxopropoxy]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide
higher cytotoxic effect
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-3-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-3-oxo-2-[[(3-pyridin-4-ylphenyl)sulfonyl]amino]propyl]benzenecarboximidamide
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3-[(2S)-3-[4-(4-aminobutanoyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide
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3-[(2S)-3-[4-(b-alanyl)piperidin-1-yl]-3-oxo-2-([[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]amino)propoxy]benzenecarboximidamide
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3-[(2S)-3-[4-(N-carbamimidoyl-b-alanyl)piperazin-1-yl]-3-oxo-2-([[2,4,6-tris(1-methylethyl)phenyl]sulfonyl]amino)propyl]benzenecarboximidamide
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3-[3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropyl]benzenecarboximidamide
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4,4'-((5-(1,2,3,4-tetrahydroisoquinoline-2-carbonyl)-1,3-phenylene)bis(oxy))dibenzimidamide
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4,4'-((5-(4-(2-aminoethyl)piperidine-1-carbonyl)-1,3-phenylene)bis(oxy))dibenzimidamide
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4,4'-((5-(4-fluorophenylsulfonamido)-1,3-phenylene)bis(oxy))dibenzimidamide
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4,4'-((5-(decahydroquinoline-1-carbonyl)-1,3-phenylene)bis(oxy))dibenzimidamide
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4,4'-((5-(naphthalene-2-sulfonamido)-1,3-phenylene)bis(oxy))dibenzimidamide
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4,4'-[(3-[[(4-fluorophenyl)sulfonyl]amino]pyridine-2,6-diyl)bis(oxy)]dibenzenecarboximidamide
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4,4'-[benzene-1,4-diylbis(oxy)]dibenzenecarboximidamide
binding structure, overview
4-(1-[3-carbamimidoyl-N-[(3-pyrrolidin-1-ylphenyl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
-
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4-(1-[3-carbamimidoyl-N-[(4'-ethoxybiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
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4-(1-[3-carbamimidoyl-N-[(4'-ethylbiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
4-(1-[N-[(4'-tert-butylbiphenyl-3-yl)sulfonyl]-3-carbamimidoyl-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
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4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
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inhibition of IGFBP-rP1 processing
4-([1-[(2S)-3-(3-carbamimidoylphenyl)-2-([[2,4,6-tris(1-methylethyl)phenyl]sulfonyl]amino)propanoyl]piperidin-4-yl]carbonyl)piperidine-1-carboximidamide
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4-([1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[(4-cyclohexylphenyl)sulfonyl]amino]propanoyl]piperidin-4-yl]carbonyl)piperidine-1-carboximidamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitor reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
4-aminobenzamidine
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weak competitive inhibition, competition assay with antibody inhibitors, overview
4-[(2-[[(2S)-6-carbamimidamido-1-oxohexan-2-yl]amino]-2-oxoethyl)carbamoyl]-6-methoxy-6-oxo-4-[3-(prop-1-en-2-yl)benzyl]hexanoic acid
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4-[1-(3-carbamimidoyl-N-[[3-(1H-imidazol-1-yl)phenyl]sulfonyl]-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(3-carbamimidoyl-N-[[3-(2-oxopiperazin-1-yl)phenyl]sulfonyl]-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(3-carbamimidoyl-N-[[3-(2-oxopiperidin-1-yl)phenyl]sulfonyl]-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(3-carbamimidoyl-N-[[3-(6-oxopyridazin-1(6H)-yl)phenyl]sulfonyl]-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(N-[[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(N-[[3-(6-aminopyridin-3-yl)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]-N-methylbutanamide
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4-[1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]butanamide
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4-[1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]butanoic acid
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4-[4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazin-1-yl]-N-methyl-4-oxobutanamide
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9-fluorenylmethyloxycarbonyl-GR-ketobenzothiazole
potent and selective inhibitor for matriptase over hepsin
anti-matriptase LDL receptor domain 3-specific monoclonal antibodies
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complete inhibition of enzyme activation
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antisense-matripase
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significantly reduces matripase protein expression by 70-80%, anti-tumoral activity on HRA cells intraperitoneal injected into nude mice
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benzyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate
benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide bis(trifluoroacetate)
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benzylsulfonyl-D-arginyl-proline-(4-amidinobenzyl)amide bis-(trifluoroacetate)
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benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide
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CJ-730
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3-amidinophenylalanine-based inhibitor CJ-730, completely inhibits pro-HGF activation in PC3 cells
D-hTyr-Ala-4-amidinobenzylamide
compound has a 10fold reduced activity against thrombin and factor Xa
ethyl (3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)carbamate
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ethyl 4-(3,5-bis(4-carbamimidoylphenoxy)benzamido)piperidine-1-carboxylate
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ethyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate
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GAVCPKILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGACPKILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGRCPKALKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGRCPKILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCAKILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPAILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKALKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKIAKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILAKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILKACRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILKKCRRDSDCPGACICRGAGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILKKCRRDSDCPGACICRGNGACGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILKKCRRDSDCPGACICRGNGYCASGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKILKKCRRDSDCPGACICRGNGYCGAGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPKRLKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
GGVCPRILKKCRRDSDCPGACICRGNGYCGSGSD
a mutant of Momordica cochinchinensis trypsin inhibitor-II
hepatcyte growth factor activator inhibitor-1
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in normal skin matriptase is complexed to hepatcyte growth factor activator inhibitor-1 wheras in squamous cell carcinoma the enzyme is present in an unassociated form
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hepatocyte growth factor activator inhibitor type 1
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physiological inhibitor of matriptase. Hepatocyte growth factor activator inhibitor type 1 (HAI-1) is required for the extracellular appearance of the protease in an expression system using a monkey kidney COS-1 cell line. In COS-1 cells co-expressing a variant form of HAI-1 without the responsible inhibition domain, matriptase does not appear in the conditioned medium
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L-arginyl-L-glutaminyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-hydroxypentan-2-yl]-L-alaninamide
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L-arginyl-N1-[(2S)-1-[[(2R)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
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L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
L-arginyl-N1-[(2S)-1-[[(2S)-6-amino-1-(1,3-benzothiazol-2-yl)-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
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methyl (2R)-1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-2-carboxylate
-
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methyl (2S)-1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidine-2-carboxylate
-
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methyl 4-[1-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperidin-4-yl]butanoate
-
-
N-((1r,4r)-4-aminocyclohexyl)-3,5-bis((3-carbamimidoylbenzyl)oxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3,5-bis((4-carbamimidoylbenzyl)oxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-((3-carbamimidoylbenzyl)oxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-((4-bromobenzyl)oxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-((4-carbamimidoylbenzyl)oxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-((6-aminopyridin-3-yl)oxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-((6-bromopyridin-3-yl)methoxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-(4-(3-aminopropanamido)phenoxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-(4-(aminomethyl)phenoxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-(4-aminophenoxy)-5-(4-carbamimidoylphenoxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-(4-carbamimidoylphenoxy)-5-((4-chlorobenzyl)oxy)benzamide
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N-((1r,4r)-4-aminocyclohexyl)-3-(4-carbamimidoylphenoxy)-5-(4-carbamoylphenoxy)benzamide
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N-(1-(3-aminopropyl)piperidin-4-yl)-3,5-bis(4-carbamimidoylphenoxy)benzamide
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N-(2-aminoethyl)-1-(3-carbamimidoyl-N-[[2,4,6-tris(1-methylethyl)phenyl]sulfonyl]-L-phenylalanyl)piperidine-4-carboxamide
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N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)-1-(2-hydroxyethyl)piperidine-4-carboxamide
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N-(3-[[(1R)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)ethyl]sulfamoyl]phenyl)-beta-alaninamide
-
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N-(3-[[(1S)-1-(3-carbamimidoylbenzyl)-2-(2-methylpiperidin-1-yl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-1-(3-carbamimidoylbenzyl)-2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-1-(3-carbamimidoylbenzyl)-2-oxo-2-piperazin-1-ylethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-1-(3-carbamimidoylbenzyl)-2-oxo-2-piperidin-1-ylethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-1-(3-carbamimidoylbenzyl)-2-[4-[4-(methylamino)-4-oxobutyl]piperidin-1-yl]-2-oxoethyl]sulfamoyl]phenyl)azetidine-3-carboxamide
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N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-3-phenylpropyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-1-[[4-(2-aminoethyl)piperidin-1-yl]carbonyl]-4-phenylbutyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-2-(4-benzylpiperidin-1-yl)-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-3-hydroxypropanamide
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N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-b-alaninamide
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N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)azetidine-3-carboxamide
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N-(3-[[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)propanamide
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N-(3-[[(1S)-2-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)-2-oxoethyl]sulfamoyl]phenyl)-beta-alaninamide
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N-(3-[[(2S)-1-[4-(2-aminoethyl)piperidin-1-yl]-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl]sulfamoyl]phenyl)-beta-alaninamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
N-(3-[[(2S)-3-(3-carbamimidoylphenyl)-1-oxo-1-(piperazin-1-yl)propan-2-yl]sulfamoyl]phenyl)-beta-alaninamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
N-(4-aminocyclohexyl)-O-(3-carbamimidoylphenyl)-N2-(naphthalen-2-ylsulfonyl)-L-serinamide
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N-(benzylsulfonyl)-3-cyclohexylalanyl-N-(4-carbamimidoylbenzyl)-L-prolinamide
inhibitor modeling in the wild-type enzyme active site, overview
N-(benzylsulfonyl)-3-cyclohexylalanyl-N-[2-(aminomethyl)-5-chlorobenzyl]-L-prolinamide
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N-[(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]-4'-methoxybiphenyl-3-sulfonamide
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N-[3-([(1S)-1-(3-carbamimidoylbenzyl)-2-[4-(4-hydroxyphenyl)piperazin-1-yl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
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N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-benzyl-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
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N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[3-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
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N-[3-([(1S)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-[4-(aminomethyl)benzyl]-2-oxoethyl]sulfamoyl)phenyl]-beta-alaninamide
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N-[3-([1-[4-(2-aminoethyl)piperidin-1-yl]-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl]sulfamoyl)phenyl]-b-alaninamide
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N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
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N2-(benzylsulfonyl)arginyl-N-(4-carbamimidoylbenzyl)-L-prolinamide
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N2-(benzylsulfonyl)arginyl-N-[2-(aminomethyl)-5-chlorobenzyl]-L-prolinamide
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O-(3-carbamimidoylphenyl)-N-(4-methylcyclohexyl)-N2-(naphthalen-2-ylsulfonyl)-L-serinamide
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R1K'4-eglin
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different eglin c variants with differing inhibitory potential versus matriptase, construction, expression and purification of eglin c variants and screening for inhibitory potency, overview, R1K'4-eglin has the wild-type Pro45 at P1 position and Tyr49 at P4' position residues replaced with Arg and Lys, respectively, leads to the production of a selective, high affinity and proteolytically stable inhibitor of matriptase, molecular modeling of enzyme-inhibitor complex, overview
R1K4-eglin
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wild type eglin c with Pro45 at P1 position and Tyr49 residues at P4 position replaced with Arg and Lys respectively, most potent, selective, high affinity and proteolytically stable inhibitor
R4R1-eglin
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with substituted P42 and L45 for arginine residues, variants containing an Arg or Lys at position 49 instead of the original Tyr residue show enhanced inhibition
scFv antibody E2
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competitive mechanism of inhibition of the scFv antibody enzyme inhibitors, which competes with substrate binding in the S1 site, the antibody binds to a number of residues flanking the active site, forming a unique three-dimensional binding epitope
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scFv antibody S4
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competitive mechanism of inhibition of the scFv antibody enzyme inhibitors, which competes with substrate binding in the S1 site, the antibody binds to a number of residues flanking the active site, forming a unique three-dimensional binding epitope
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SFTI1
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serine protease inhibitor can only inhibit Epi/MTP and cathepsin G. Mammary epithelial growth and morphogenesis in the presence of the latent form hepatocyte growth factor (pro-HGF) is blocked by addition of SFTI1 an inhibitor of the Epi/MTP protease activity
sulfated 3-amidinophenylalanine derivatives
deiverse variants, overview
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
4-(1-[3-carbamimidoyl-N-[(4'-ethylbiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
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4-(1-[3-carbamimidoyl-N-[(4'-ethylbiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
benzyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate
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benzyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate
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inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1
hepatocyte growth factor activator inhibitor
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HAI-1, the cognate transmembrane inhibitor of the enzyme, which is coexpressed with matriptase in epithelium
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hepatocyte growth factor activator inhibitor
HAI-1, conventional protease inhibitor
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hepatocyte growth factor activator inhibitor
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active protease is inhibited by, and forms complexes with, hepatocyte growth factor activator inhibitor (HAI-1)
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hepatocyte growth factor activator inhibitor 1
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following matriptase activation, the active enzyme is immediately inhibited by binding to hepatocyte growth factor activator inhibitor 1, resulting in stable matriptase-hepatocyte growth factor activator inhibitor 1 complexes that are rapidly secreted
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hepatocyte growth factor activator inhibitor 1
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HAI-1, a Kunitz-type inhibitor that functions both as a chaperone and a reversible inhibitor
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hepatocyte growth factor activator inhibitor type I
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inhibition activities of a cell membrane-anchored form of recombinant HAI-1 (maHAI-1) against different matriptase variants in the hydrolysis of peptidyl-4-methyl-coumaryl-7-amide (MCA) substrates are compared: stem domain of matriptase affects the interaction between this protease and HAI-1
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hepatocyte growth factor activator inhibitor type I
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hepatocyte growth factor activator inhibitor type I (HAI-1) is shown to be required for the extracellular appearance of matriptase using COS-1 cells. Co-expression of recombinant variants of HAI-1 with the inhibition activity toward matriptase, including a variant consisting only of Kunitz domain I (the domain responsible for inhibition of matriptase), allows for the appearance of matriptase in the conditioned medium, whereas that of the variants without the inhibitory activity does not
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hepatocyte growth factor activator inhibitor-1
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Hai1a, i.e. Spint1Ia, enzyme inactivation by HAI-1 is required for epithelial integrity of the zebrafish epidermis, inhibitor mutant zebrafish show disrupted epidermal integrity, enhanced upon combined loss of hai1a and the paralogue hai1b, overview
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hepatocyte growth factor activator inhibitor-1
i.e. HAI-1, binding is reversible and acid labile
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hepatocyte growth factor activator inhibitor-1
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HAI-1, forms complexes wih the enzyme in vivo
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hepatocyte growth factor activator inhibitor-1
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is required for proper development of placenta, overview
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hepatocyte growth factor activator inhibitor-1
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HAI-1, a Kunitz-type transmembrane serine protease inhibitor, cognate inhibitor of matriptase with regulatory function, molecular mechanism of inhibition, domain structure of HAI-1, proteolytic processing during maturation, activation, and shedding, enzyme-inhibitor complex structure, overview, the level of HAI-1 expression seems to be an important factor in the regulation of matriptase zymogen activation
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hepatocyte growth factor activator inhibitor-1
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HAI-1, without HAI-1 active matriptase may become unstable, leading to its degradation and low protein expression
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hepatocyte growth factor activator inhibitor-1
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activated matriptase is immediately inhibited by and forms complex with hepatocyte growth factor activator inhibitor-1
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hepatocyte growth factor activator inhibitor-1
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HAI-1, the cognate matriptase inhibitor is able to compensate for the effect of augmented matriptase activity, providing a rationale for the inhibition of matriptase to prevent tumor growth in vivo
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hepatocyte growth factor activator inhibitor-1
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is required for proper development of placenta, overview
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hepatocyte growth factor activator inhibitor-1
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HAI-1, a Kunitz-type transmembrane serine protease inhibitor, complex formation with the enzyme, enzyme inhibition is essential for placental development, overview
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hepatocyte growth factor activator inhibitor-1
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HAI-1, an extremely effective inhibitor of matriptase in vitro, that has a high affinity for matriptase binding and is typically co-expressed with matriptase in vivo. Matriptase activation appears to require physical interaction with its related inhibitor, HAI-1, which may serve to protect against aberrant matriptase proteolysis. Deletion or mutation of the LDLA domain of HAI-1 results in both a reduction in surface matriptase expression and abolishment of matriptase activity
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L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
docking of the inhibitor in the active site of matriptase, structure, overview
L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
EC50 is 0.00564-0.0068 mM, the inhibitor contains a ketobenzothiazole serine trap designed based on matriptase's auto-catalytic domain (RQAR), it is a selective, slow, tight-binding inhibitor of matriptase that significantly reduces viral replication of H1N1 influenza virus, including the 2009 pandemic virus
sunflower trypsin inhibitor-1
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and several derivatives with different amino acid side chains, overview
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
additional information
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no inhibition of IGFBP-rP1 processing by leupeptin, pepstatin, and N-(R)-(2-(hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-l-3-(2'-naphthyl)alaninyl-l-alanine 2-aminoethyl amide, i.e. TAPI-1; not inhibited by leupeptin, pepstatin and N-(R)-(2-(hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-3-(2'-naphthyl)alaninyl-L-alanine 2-aminoethyl amide
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additional information
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inhibition of matriptase activation in vitro and in vivo, overview
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additional information
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inhibitor design and synthesis, inhibitory potency and structure-activity relationships, overview, matriptase blockade could potentially modulate tumorigenesis and metastasis in vivo
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additional information
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autoinhibitory role of the LDLRA modules that may prevent premature activation of matriptase in the absence of appropriate activation stimuli
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additional information
controlled by a serpin complex, consisting of antithrombin III, alpha1-antitrypsin and alpha2-antiplasmin
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additional information
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controlled by a serpin complex, consisting of antithrombin III, alpha1-antitrypsin and alpha2-antiplasmin
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additional information
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the enzyme is competitively inhibited by the anti-MT-SP1 antibody FabE2
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additional information
design and synthesis of potent, selective inhibitors of matriptase, overview. Design of a class of potent and selective peptidomimetic inhibitors of matriptase based on the P4-P1 (Arg-Gln-Ala-Arg) portion of the activation peptide of matriptase, to which is linked a C-terminal serine trap in the form of a ketobenzothiazole group. The ketobenzothiazole serine trap is selected to form a covalent and reversible bond with the catalytic serine residue of the enzyme. Importance of stereochemistry at the P1 position for inhibitory potency
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additional information
O-(3-carbamimidoylphenyl)-L-serine amides as matriptase inhibitors, overview. Analysis of cytotoxic effects of inhibitors
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additional information
inhibitor design, synthesis of diverse 5-substituted phenylene1,3-bis(oxy) dibenzimidamide analogues, overview. Anaysis of cytotoxic effects of inhibitors
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additional information
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inhibitor design, synthesis of diverse 5-substituted phenylene1,3-bis(oxy) dibenzimidamide analogues, overview. Anaysis of cytotoxic effects of inhibitors
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additional information
analysis of interaction of matriptase-2 with prototype low-molecular weight ligands using site-directed mutagenesis, kinetic analysis and molecular modeling, substrate/inhibitor-enzyme interactions, overview
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additional information
analysis of interaction of matriptase-2 with prototype low-molecular weight ligands using site-directed mutagenesis, kinetic analysis and molecular modeling, substrate/inhibitor-enzyme interactions, overview
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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
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additional information
peptide inhibitor docking study with matriptase and matriptase-2, overview
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additional information
generation of monoclonal antibodies against mutant N164Q/R614A and use as inhibitors. Two antibodies are competitive inhibitors and able to block the activity of wild-type full-length matriptase in complex biological samples by binding near the active site
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additional information
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generation of monoclonal antibodies against mutant N164Q/R614A and use as inhibitors. Two antibodies are competitive inhibitors and able to block the activity of wild-type full-length matriptase in complex biological samples by binding near the active site
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