3.4.21.20: cathepsin G
This is an abbreviated version!
For detailed information about cathepsin G, go to the full flat file.
Word Map on EC 3.4.21.20
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3.4.21.20
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elastase
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neutrophil
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leukocyte
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proteinases
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granule
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polymorphonuclear
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myeloperoxidase
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chymase
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granulocyte
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thrombin
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platelet
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mast
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azurophilic
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serpins
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plasmin
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lactoferrin
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collagenase
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neutrophil-derived
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granzyme
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kallikrein
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1-proteinase
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degranulation
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tryptase
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antineutrophil
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1-antichymotrypsin
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eglin
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drug development
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nsp4
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antiproteinases
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2-macroglobulin
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fmlp
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hne
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alpha-chymotrypsin
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wegener
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chediak-higashi
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antiprotease
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elastolytic
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chymostatin
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slpi
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elastase-like
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p-anca
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procollagenase
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alpha1-proteinase
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pharmacology
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pmn-derived
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elafin
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1-antitrypsin
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medicine
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granulomatosis
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alpha1-antichymotrypsin
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anti-cathepsin
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neutrophil-mediated
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anca-positive
- 3.4.21.20
- elastase
- neutrophil
- leukocyte
- proteinases
- granule
-
polymorphonuclear
- myeloperoxidase
- chymase
- granulocyte
- thrombin
- platelet
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mast
-
azurophilic
- serpins
- plasmin
- lactoferrin
- collagenase
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neutrophil-derived
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granzyme
- kallikrein
-
1-proteinase
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degranulation
- tryptase
-
antineutrophil
-
1-antichymotrypsin
- eglin
- drug development
- nsp4
-
antiproteinases
-
2-macroglobulin
- fmlp
- hne
- alpha-chymotrypsin
-
wegener
-
chediak-higashi
-
antiprotease
-
elastolytic
- chymostatin
- slpi
-
elastase-like
-
p-anca
- procollagenase
- alpha1-proteinase
- pharmacology
-
pmn-derived
- elafin
-
1-antitrypsin
- medicine
-
granulomatosis
- alpha1-antichymotrypsin
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anti-cathepsin
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neutrophil-mediated
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anca-positive
Reaction
specificity similar to chymotrypsin C =
Synonyms
alpha-protease, cat G, Cat-G, Cat.G, CatG, Cath G, cathepsin G, chymotrypsin-like proteinase, CTSG, More, neutral proteinase, serine protease cathepsin G, Vimentin-specific protease, VSP
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Inhibitors
Inhibitors on EC 3.4.21.20 - cathepsin G
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11-oxo-beta-boswellic acid
0.01 mM, 30% cathepsin G activity compared to control
2-amino-3,1-benzoxazin-4-ones
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non-covalent complex formation, hydrophobic and basic residues at position 2, kinetics of acylation and desacylation, binding at the enzyme's active site
3-O-acetyl-11-oxo-beta-boswellic acid
0.01 mM, 15% cathepsin G activity compared to control
3-O-acetyl-beta-boswellic acid
0.01 mM, 5% cathepsin G activity compared to control
6-((1'R,2'S,5'R)-menthyloxycarbonyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
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6-((1'S)-camphanyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
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selective inhibition
6-((1'S,2'R,5'S)-menthyloxycarbonyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
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6-(benzoyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
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selective inhibition
6-(N-tosyl-L-phenylalanyl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-dione
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beta-boswellic acid
0.01 mM, 30% cathepsin G activity compared to control
bis(4-ethylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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bis(4-methoxyphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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more potent inhibitor for related proteases than cathepsin G
bis(4-methylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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bis(4-tert-butylphenyl) [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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bis-naphthyl beta-ketophosphoric acid
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moderately potent, competitive, reversible, the R-isomer occupies the active site of the enzyme
bis[4-(1,1,3,3-tetramethylbutyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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3% inhibition, 115 microM
bis[4-(1-methylethyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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bis[4-(methylsulfanyl)phenyl] ([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][(O-tert-butyl-L-threonyl)amino]methyl)phosphonate
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bis[4-(methylsulfanyl)phenyl] [[4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl]([O-tert-butyl-N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-threonyl]amino)methyl]phosphonate
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bis[4-(methylsulfanyl)phenyl] [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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more potent inhibitor for related proteases than cathepsin G
dermatan sulfate
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25 kDa, protection of laminin and fibronectin against degradation by cathepsin G
dinaphthalen-2-yl [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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diphenyl (1-[[(benzyloxy)carbonyl]amino]-3-carbamimidamidopropyl)phosphonate
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diphenyl (4-amino-1-[[(benzyloxy)carbonyl]amino]butyl)phosphonate
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5% inhibition, 221 microM
diphenyl [[[(benzyloxy)carbonyl]amino](4-carbamimidamidophenyl)methyl]phosphonate
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more potent inhibitor for related proteases than cathepsin G
diphenyl [[[(benzyloxy)carbonyl]amino](4-carbamimidoylphenyl)methyl]phosphonate
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30% inhibition, 112 microM
diphenyl [[[(benzyloxy)carbonyl]amino](6-carbamimidoylnaphthalen-2-yl)methyl]phosphonate
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5% inhibition, 112 microM
diphenyl [[[(benzyloxy)carbonyl]amino](phenyl)methyl]phosphonate
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more potent inhibitor for related proteases than cathepsin G
glut-11-oxo-beta-boswellic acid
0.01 mM 20% cathepsin G activity compared to control
heparan sulfate
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60 kDa, protection of laminin and fibronectin against degradation by cathepsin G
heparin
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12 kDa, 1:1 binding stoichiometry with cathepsin G, protection of laminin and fibronectin against degradation by cathepsin G
high molecular mass kininogen
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i.e. HK, human, competitive, inhibits platelet activation by the enzyme completely by complex formation with the enzyme
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JNJ-10311795
inhibitor of cathepsin G and chymase. The possibility to inhibit both cathepsin G and chymase with a single molecule suggests an opportunity in the treatment of asthma and chronic obstructive pulmonary disease
L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
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L-valyl-N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
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N-acetyl-L-phenylalanyl-L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
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N-acetyl-L-phenylalanyl-L-valyl-N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
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N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe-chloromethylketone
irreversible inhibitor
N-succinyl-L-Val-L-Pro-L-Phe(OPh)2
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irreversible CatG inhibitor, complete inhibition at 0.01 mM
N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-valyl-N-([4-[bis(tert-butoxycarbonyl)carbamimidamido]phenyl][bis[4-(methylsulfanyl)phenoxy]phosphoryl]methyl)-O-tert-butyl-L-threoninamide
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N-[[bis[4-(methylsulfanyl)phenoxy]phosphoryl](4-carbamimidamidophenyl)methyl]-L-threoninamide
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two times more active against cathepsin G than against trypsin
RG1150
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i.e. carboxymethyl-benzylamide-dextran derivative, protection of laminin and fibronectin against degradation by cathepsin G
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RG1192
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i.e. carboxymethyl-benzylamide-dextran sulfate derivative, protection of laminin and fibronectin against degradation by cathepsin G
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RG1503
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i.e. carboxymethyl-dextran sulfate derivative, protection of laminin and fibronectin against degradation by cathepsin G
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[2-(3-methylcarbamoyl-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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[2-(3-[(3-benzoylamino-propyl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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[2-(3-[(piperidin-4-yl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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reversible, selective, competitive inhibition
[2-(3-[methyl-(diphenyl-ethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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strong inhibition
[2-(3-[methyl-(phenethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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[2-(3-[methyl[1-(2-naphthoyl)piperidin-4-yl]amino]carbonyl]-2-naphthyl)-1-(1-naphthyl)-2-oxoethyl]phosphonic acid
0.0005 mM, 10% cathepsin G activity compared to control
[2-[3-(benzyl-methyl-carbamoyl)-naphthalen-2-yl]-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid
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alpha1-Aantichymotrypsin
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acute phase reactant which is up-regulated during inflammation episodes to compensate for the excess of enzymes released from the actvated neutrophils
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benzyloxycarbonyl-Gly-Leu-Phe-chloromethyl ketone
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i.e. CK-08, specific for cathepsin G
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TPCK, inhibitor of the proteolytic activity of cathepsin G, effectively eliminated cathepsin G-induced chemotaxis of monocytes
N-tosyl-L-phenylalanine chloromethyl ketone
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TPCK, inhibitor of the proteolytic activity of cathepsin G, effectively eliminated cathepsin G-induced chemotaxis of monocytes
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effectively inhibited the action of cathepsin G against the substrate at a concentration of 1 mmol/l
Na-tosyl-Phe-chloromethylketone
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inhibition of Cathepsin G reduces tumor vascularity
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reversible CatG inhibitor, complete inhibition at 0.01 mM
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complete inhibition at 0.2 mM after 30 min at 25°C
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no inhibition by EDTA and leupeptin both at 0.1 mM
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additional information
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5kD heparin fragment protects against inhibition by alpha1-antichymotrypsin inhibitor, eglin c and alpha1-proteinase inhibitor; kinetic mechanism of inhibition
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additional information
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inhibition mechanism and kinetics, effect of ionic strength
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additional information
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structural features of inhibition, high-throughput screening of a diverse chemical library, lead structure is bis-naphthyl beta-ketophosphoric acid
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additional information
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no inhibitory effect: diphenyl (1-[[(benzyloxy)carbonyl]amino]-4-carbamimidamidobutyl)phosphonate
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additional information
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when microglia are treated with interferon-gamma to mimic a T helper type 1-biased cytokine milieu in multiple sclerosis, CatG is drastically down-regulated resulting in significantly increased stability of myelin basic protein and a selective lack of CatG-derived proteolytic fragments, inhibition of serine proteases eliminates differences in lysosomal MBP-processing between resting and IFN-gamma-stimulated microglia
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additional information
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wild type mouse cathepsin G is not inhibited by Lys16-aprotinin
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