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Literature summary for 3.4.21.37 extracted from
- Synthetic inhibitors of elastase (1994), Med. Res. Rev., 14, 127-194.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | the enzyme has been implicated in the promotion or exacerbation of a number of diseases including pancreatitis acute respiratory distress syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema and cystic fibrosis. During the last decade, an intense effort has been directed towards the development of inhibitors to supplement the body elastase inhibitory capacity and thereby shift the proteinase/antiproteinase imbalance in pathogenic conditions. Several of these inhibitors have been produced by recombinant technology and formulations have been developed for aerosol and/or intravenous administration. The review focuses on low molecular-weight, synthetic inhibitors. A very small percentage of compounds possess all the necessary properties, including lack of toxicity, for progression into the clinic. ICI 200,880 has many of the desired characteristics of a drug to treat the diseases associated with human neutrophil elastase: chemical stability, in vitro and in vivo activity, a long duration of action and adequate metabolic stability. Currently ICI 200,880 is the only low molecular-weight inhibitor for neutrophil elastase known to be undergoing clinical trials, and may be the compound which finally demonstrates, the clinical utility of a synthetic neutrophil elastase inhibitor | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ((6R,7S)-2-{[(2S)-2-(dihydroxymethyl)pyrrolidin-1-yl]carbonyl}-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)methyl acetate | - |
Homo sapiens |  |
| (1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methyl 2,6-dichlorobenzoate | - |
Homo sapiens | |
| (1-{1-Methyl-2-oxo-2-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-ethylcarbamoyl}-ethyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (1-{2-[1-(4,5-Dihydro-oxazole-2-carbonyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (1-{2-[1-(Benzooxazol-2-yl-hydroxy-methyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (1-{2-[1-(Benzooxazole-2-carbonyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (1-{2-[2-(3,3-Difluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (1-{[1-(2-tert-Butoxycarbonylamino-3-methyl-butyryl)-pyrrolidine-2-carbonyl]-amino}-2-methyl-propyl)-phosphonic acid diphenyl ester | - |
Homo sapiens | |
| (2-(3,5-difluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (2S)-1-({(6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-yl}carbonyl)pyrrolidine-2-carboxylic acid | - |
Homo sapiens | |
| (4-tert-butyl-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methyl 2,6-dichlorobenzoate | - |
Homo sapiens | |
| (5-Benzyloxycarbonylamino-1-{2-methyl-1-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propylcarbamoyl}-pentyl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| (5E)-3-benzyl-5-but-2-ynylidenedihydrofuran-2(3H)-one | - |
Homo sapiens | |
| (5E)-3-benzyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one | - |
Homo sapiens | |
| (5E)-3-butyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one | - |
Homo sapiens | |
| (5E)-5-prop-2-ynylidenedihydrofuran-2(3H)-one | - |
Homo sapiens | |
| (5Z)-3-benzyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one | - |
Homo sapiens | |
| (6E)-3-benzyl-6-prop-2-ynylidenetetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| (6E)-6-(1-bromoethylidene)-3-isopropyltetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| (6E)-6-(bromomethylene)-3-isopropyltetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| (6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid 5,5-dioxide | - |
Homo sapiens | |
| (6Z)-3-benzyl-6-prop-2-ynylidenetetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| (6Z)-6-(bromomethylene)-3-isopropyltetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| 1-(2-Acetylamino-propionyl)-pyrrolidine-2-carboxylic acid (3-chloro-1-methyl-2-oxo-propyl)-amide | - |
Homo sapiens | |
| 1-methyl-1H-tetrazole-5-thiol | - |
Homo sapiens | |
| 1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid (3-chloro-1-isopropyl-2-oxo-propyl)-amide | - |
Homo sapiens | |
| 1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid (3-chloro-1-methyl-2-oxo-propyl)-amide | - |
Homo sapiens | |
| 1-[2-(4-Benzenesulfonylaminocarbonyl-benzoylamino)-3-methyl-butyryl]-pyrrolidine-2-carboxylic acid (3,3-difluoro-1-isopropyl-2-oxo-3-phenethylcarbamoyl-propyl)-amide | - |
Homo sapiens | |
| 1-[2-(chloromethyl)phenyl]-3,3-difluoroazetidin-2-one | - |
Homo sapiens | |
| 1-{2-[4-(4-Bromo-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (3,3,3-trifluoro-1-isopropyl-2-oxo-propyl)-amide | - |
Homo sapiens | |
| 1-{2-[4-(4-Chloro-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (1-isopropyl-2,3-dioxo-heptyl)-amide | - |
Homo sapiens | |
| 1-{2-[4-(4-Chloro-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (3,3,3-trifluoro-1-isopropyl-2-oxo-propyl)-amide | - |
Homo sapiens | |
| 1-{3-Methyl-2-[(naphthalene-2-carbonyl)-amino]-butyryl}-pyrrolidine-2-carboxylic acid (1-isopropyl-2,3-dioxo-heptyl)-amide | - |
Homo sapiens | |
| 1-{[({2-[3-(trifluoromethyl)phenyl]ethyl}amino)carbonyl]oxy}pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 2,2-Dimethyl-propionic acid 4-[2-(2,2-dihydroxy-ethylcarbamoyl)-benzenesulfonylamino]-phenyl ester | - |
Homo sapiens | |
| 2,2-Dimethyl-propionic acid 4-[4-(2,2-dimethyl-propionyloxy)-benzoyl]-phenyl ester | - |
Homo sapiens | |
| 2-(2,4-dinitrophenyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide | - |
Homo sapiens | |
| 2-(2-ethylbutanoyl)-1,2-benzisothiazol-3(2H)-one | - |
Homo sapiens | |
| 2-(2-furoyl)-1,2-benzisothiazol-3(2H)-one | - |
Homo sapiens | |
| 2-(2-furoyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide | - |
Homo sapiens | |
| 2-(3,3,3-Trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carboxylic acid benzyl ester | - |
Homo sapiens | |
| 2-(4-Chloro-benzenesulfonylamino)-5,5-dihydroxy-pentanoic acid (2-isopropylamino-5-methyl-4-oxo-4H-benzo[d][1,3]oxazin-7-yl)-amide | - |
Homo sapiens | |
| 2-(4-Dihydroxymethyl-phenoxy)-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid 4-methyl-benzylamide | - |
Homo sapiens | |
| 2-(chloromethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide | - |
Homo sapiens | |
| 2-(trifluoromethyl)-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-Acetylamino-N-(1-ethylcarbamoyl-ethyl)-propionamide | - |
Homo sapiens | |
| 2-Acetylamino-N-[1-(3-chloro-1-methyl-2-oxo-propylcarbamoyl)-ethyl]-propionamide | - |
Homo sapiens | |
| 2-Acetylamino-N-[2-(2-{2-[(2-chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethyl]-propionamide | - |
Homo sapiens | |
| 2-Acetylamino-N-{1-[1-(3-chloro-1-methyl-2-oxo-propylcarbamoyl)-ethylcarbamoyl]-ethyl}-propionamide | - |
Homo sapiens | |
| 2-amino-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-amino-5-ethyl-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-benzoyl-1,2-benzisothiazol-3(2H)-one 1,1-dioxide | - |
Homo sapiens | |
| 2-CF3CF2C(O)NH-C6H4-SO2-F | - |
Homo sapiens | |
| 2-CF3SNH-C6H4-SO2-F | - |
Homo sapiens | |
| 2-ethoxy-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-ethoxy-5-ethyl-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-methyl-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 2-nitrophenylboronic acid | - |
Homo sapiens | |
| 2-[(Imidazole-1-carbonyl)-amino]-pentanoic acid methyl ester | - |
Homo sapiens | |
| 2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid (1-benzo[1,3]dioxol-5-yl-butyl)-amide | - |
Homo sapiens | |
| 2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid (1-p-tolyl-butyl)-amide | - |
Homo sapiens | |
| 2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid 4-methyl-benzylamide | - |
Homo sapiens | |
| 2-[benzyloxycarbonyl-NHCH2-C(O)NH]-C6H4-SO2-F | - |
Homo sapiens | |
| 3,4-dichloro-1H-isochromen-1-one | - |
Homo sapiens | |
| 3-benzyl-1-(sulfooxy)pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-benzyl-1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-benzyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-CF3-C6H4-CO-Ala-Ala-4-nitroanilide | - |
Homo sapiens | |
| 3-chloro-1H-isochromen-1-one | - |
Homo sapiens | |
| 3-isopropyl-1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-isopropyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-isopropyl-6-methylenetetrahydro-2H-pyran-2-one | - |
Homo sapiens | |
| 3-methoxy-1-oxo-1H-isochromen-7-yl nitrite | - |
Homo sapiens | |
| 3-methoxy-7-nitro-1H-isochromen-1-one | - |
Homo sapiens | |
| 3-tert-butyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione | - |
Homo sapiens | |
| 3-[(1-{2-[2-(3-Methoxycarbonyl-propionylamino)-propionylamino]-propionyl}-pyrrolidine-2-carbonyl)-amino]-4-methyl-2-oxo-pentanoic acid methyl ester | - |
Homo sapiens | |
| 3-[2-(2-Benzyloxycarbonylamino-propionylamino)-propionylamino]-2-oxo-pentanoic acid benzyl ester | - |
Homo sapiens | |
| 3-{[1-(2-Benzyloxycarbonylamino-3-methyl-butyryl)-pyrrolidine-2-carbonyl]-amino}-4-methyl-2-oxo-pentanoic acid ethyl ester | - |
Homo sapiens | |
| 4-CH3-C6H4-SO2-F | - |
Homo sapiens | |
| 4-chloro-3-ethoxy-1H-isochromen-1-one | - |
Homo sapiens | |
| 4-chloro-3-methoxy-1-oxo-1H-isochromen-7-yl nitrite | - |
Homo sapiens | |
| 4-chloro-3-methoxy-7-nitro-1H-isochromen-1-one | - |
Homo sapiens | |
| 4-{5-(Adamantane-1-sulfonylamino)-6-oxo-6-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-hexylcarbamoyl}-butyric acid methyl ester | - |
Homo sapiens | |
| 5-(2-Chloro-benzyl)-2-(2,2-dimethyl-propionyloxy)-5-hydroxy-5,6-dihydro-thieno[3,2-c]pyridin-5-ium; chloride | - |
Homo sapiens | |
| 5-(4-Chloro-benzenesulfonylamino)-5-(2-isopropylamino-5-methyl-4-oxo-4H-benzo[d][1,3]oxazin-7-ylcarbamoyl)-pentyl-ammonium; chloride | - |
Homo sapiens | |
| 5-ethyl-2-(isopropylamino)-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 5-ethyl-2-methyl-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 5-methyl-2-(trifluoromethyl)-4H-3,1-benzoxazin-4-one | - |
Homo sapiens | |
| 6-({1-[2-(2-Benzyloxycarbonylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-amino)-4,4-difluoro-5-oxo-heptanoic acid methyl ester | - |
Homo sapiens | |
| 6-amino-2-(2,2,2-trifluoro-acetylamino)-hexanoic acid [1-(4-trifluoromethyl-phenylcarbamoyl)-ethyl]-amide | - |
Homo sapiens | |
| 7-amino-3-methoxy-1H-isochromen-1-one | - |
Homo sapiens | |
| 7-amino-4-chloro-3-methoxy-1H-isochromen-1-one | - |
Homo sapiens | |
| Ac-Pro-Ala-Pro-NH2CH(CH3)CH2OH | - |
Homo sapiens | |
| Ac-Pro-Ala-Pro-NH2CH(CH3)CHO | - |
Homo sapiens | |
| Ac-Pro-Ala-Pro-NH2CH(CH3)CONH2 | - |
Homo sapiens | |
| Ala-Ala-Pro-Ala | - |
Homo sapiens | |
| benzyl 3,3,3-trifluoro-1-isopropyl-2-oxopropylcarbamate | - |
Homo sapiens | |
| Boc-Ala-Pro-isobutyl-boronic acid amide | - |
Homo sapiens | |
| Butyric acid 3-(3-bromomethylene-6-isopropyl-5-oxo-[1,4]dioxan-2-yl)-pyrrolidin-1-yl ester | - |
Homo sapiens | |
| CBZ-Ala-(isobutyl-difluoro-boron)amide | - |
Homo sapiens | |
| CBZ-Ala-isobutyl-boronic acid amide | - |
Homo sapiens | |
| CF3-CO-Ala-Ala-4-nitroanilide | - |
Homo sapiens | |
| CF3-CO-Ala-Ala-Ala-OH | - |
Homo sapiens | |
| ethyl (2S,3R)-2-[(2,2-dihydroxyethyl)sulfonyl]-3-ethyl-4-oxoazetidine-1-carboxylate | - |
Homo sapiens | |
| Formic acid 2-(3-{1-[2-(N'-benzyloxycarbonyl-N'-propyl-hydrazinocarbonyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-ureido)-4-methyl-pentyl ester | - |
Homo sapiens | |
| Formic acid 4-methyl-2-(3-{2-methyl-1-[2-(N'-phenoxycarbonyl-N'-propyl-hydrazinocarbonyl)-pyrrolidine-1-carbonyl]-propyl}-ureido)-pentyl ester | - |
Homo sapiens | |
| glutaryl-Ala-Ala-Pro-NH-C3H7 | - |
Homo sapiens | |
| m-CF3-C6H4-CO-Ala-Ala-4-nitroanilide | - |
Homo sapiens | |
| methoxsuccinyl-Ala-Ala-Pro-Ile-boronic acid | - |
Homo sapiens | |
| methoxysuccinyl-Ala-Ala-Pro-(isobutyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane)amide | - |
Homo sapiens | |
| methoxysuccinyl-Ala-Ala-Pro-isobutyl-boronic acid amide | - |
Homo sapiens | |
| methoxysuccinyl-Ala-Ala-Pro-phenylethylboronic acid | - |
Homo sapiens | |
| N'-{1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-N-methyl-hydrazinecarboxylic acid 1-benzylcarbamoyl-ethyl ester | - |
Homo sapiens | |
| N'-{1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-N-methyl-hydrazinecarboxylic acid 1-carbamoyl-ethyl ester | - |
Homo sapiens | |
| N-(1-(1-[1-(4-benzoyl-phenylcarbamoyl)-2-methyl-propylcarbamoyl]-3-methyl-butylcarbamoyl)-2-(4-hydroxy-phenyl)-ethyl)-succinamic acid | - |
Homo sapiens | |
| N-(1-{1-Methyl-2-oxo-2-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester | - |
Homo sapiens | |
| N-(1-{2-[2-(3-Chloro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester | - |
Homo sapiens | |
| N-(1-{2-[2-(4-Ethoxy-3,3-difluoro-1-isopropyl-2-oxo-butylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester | - |
Homo sapiens | |
| N-(2-phenylethyl)-1H-imidazole-1-carboxamide | - |
Homo sapiens | |
| N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-succinamic acid | - |
Homo sapiens | |
| N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-terephthalamic acid | - |
Homo sapiens | |
| N-(5-benzyloxycarbonylamino-1-(1-[2-(1-formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propylcarbamoyl)-pentyl)-succinamic acid | - |
Homo sapiens | |
| N-{1-[2-(2-{2-[(2-Chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid | - |
Homo sapiens | |
| N-{1-[2-(2-{2-[(2-Chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid methyl ester | - |
Homo sapiens | |
| N-{1-[2-(2-{2-[Isopropyl-(4-nitro-phenoxycarbonyl)-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid methyl ester | - |
Homo sapiens | |
| N-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-imidazole-1-carboxamide | - |
Homo sapiens | |
| N-{5-(Adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl}-4-dihydroxymethyl-benzamide | - |
Homo sapiens | |
| oleic acid | - |
Homo sapiens | |
| oleoyl-Ala-Ala-Pro-Ala | - |
Homo sapiens | |
| oleoyl-Ala-Ala-Pro-Val | - |
Homo sapiens | |
| phenylboronic acid | - |
Homo sapiens | |
| succinyl-Tyr-D-Leu-D-Val-4-nitroanilide | - |
Homo sapiens | |
| tert-butoxycarbonyl-Val-Val-Val-NH-(CH2)11-CH3 | - |
Homo sapiens | |
| tert-butyl (6R,7S)-3-[(acetyloxy)methyl]-7-chloro-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate 5,5-dioxide | - |
Homo sapiens | |
| tert-butyl (6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate 5,5-dioxide | - |
Homo sapiens | |
| [({(2R,3S)-3-ethyl-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidin-2-yl}carbonyl)oxy]acetic acid | - |
Homo sapiens | |
| {(6R,7S)-2-[(tert-butylamino)carbonyl]-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl}methyl acetate | - |
Homo sapiens | |
| {1-[2-(1-Acetyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {1-[2-(1-Aminooxalyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {1-[2-(1-Formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {1-[2-(1-Isopropyl-2,3-dioxo-heptylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {1-[2-(3,3-Difluoro-1-isopropyl-2,4-dioxo-7-phenyl-heptylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {1-[2-(3-Benzylcarbamoyl-3,3-difluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {2-Methyl-1-[(R)-2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {2-Methyl-1-[(S)-2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {2-Methyl-1-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
| {2-Methyl-1-[2-(3,3,3-trifluoro-2-hydroxy-1-isopropyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| azurophil granule | cytoplasmic | Homo sapiens | 42582 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | neutrophil elastase is a key component of the bodys inflammatory defenses, assisting the neutrophil in its migration to the site of inflammation and participating in the proteolytic degradation of invading microorganisms. In addition the enzyme is involved in tissue remodeling and wound healing. Under homeostatic conditions, the destructive effects of the enzyme are limited to the microenvironment immediately surrounding the neutrophil by endogenous proteinase inhibitors such as alpha1-proteinase inhibitor. As a consequence of chronic inflammation, however, the balance between the enzyme and alpha1-antitrypsin can be shifted in favor of the enzyme, resulting in uncontrolled tissue destruction. The enzyme has been implicated in the promotion or exacerbation of a number of diseases including pancreatitis acute respiratory distress syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema and cystic fibrosis | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| glycoprotein | several isoforms differing in their extent of glycosylation | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| mast cell | - |
Homo sapiens | - |
| monocyte | - |
Homo sapiens | - |
| neutrophil | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Elastin + H2O | the enzyme cleaves elastin selectively near the cross-linking desmosine residues | Homo sapiens | ? | - |
? | |
| additional information | neutrophil elastase is a key component of the bodys inflammatory defenses, assisting the neutrophil in its migration to the site of inflammation and participating in the proteolytic degradation of invading microorganisms. In addition the enzyme is involved in tissue remodeling and wound healing. Under homeostatic conditions, the destructive effects of the enzyme are limited to the microenvironment immediately surrounding the neutrophil by endogenous proteinase inhibitors such as alpha1-proteinase inhibitor. As a consequence of chronic inflammation, however, the balance between the enzyme and alpha1-antitrypsin can be shifted in favor of the enzyme, resulting in uncontrolled tissue destruction. The enzyme has been implicated in the promotion or exacerbation of a number of diseases including pancreatitis acute respiratory distress syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema and cystic fibrosis | Homo sapiens | ? | - |
? | |
| succinyl-Tyr-Leu-Val-4-nitroanilide + H2O | - |
Homo sapiens | ? | - |
? | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | overview, oligopeptide inhibitors, aldehyde inhibitors, carbamate inhibitors, carbazate inhibitors, trifluoromethylketone inhibitors, difluoromethylene inhibitors, boronic acid inhibitors, isocoumarin inhibitors, cephalosporin inhibitors, azetidinone inhibitors, benzothiazolinone inhibitors and various other classes | Homo sapiens | |
| 0.000004 | - |
1-methyl-1H-tetrazole-5-thiol | - |
Homo sapiens | |
| 0.00002 | - |
(2-(3,5-difluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester | - |
Homo sapiens | |
| 0.000025 | - |
6-amino-2-(2,2,2-trifluoro-acetylamino)-hexanoic acid [1-(4-trifluoromethyl-phenylcarbamoyl)-ethyl]-amide | - |
Homo sapiens | |
| 0.000035 | - |
N-(5-benzyloxycarbonylamino-1-(1-[2-(1-formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propylcarbamoyl)-pentyl)-succinamic acid | - |
Homo sapiens | |
| 0.00006 | - |
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-terephthalamic acid | - |
Homo sapiens | |
| 0.00007 | - |
oleoyl-Ala-Ala-Pro-Ala | - |
Homo sapiens | |
| 0.00011 | - |
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-succinamic acid | - |
Homo sapiens | |
| 0.00021 | - |
tert-butoxycarbonyl-Val-Val-Val-NH-(CH2)11-CH3 | - |
Homo sapiens | |
| 0.004 | - |
m-CF3-C6H4-CO-Ala-Ala-4-nitroanilide | - |
Homo sapiens | |
| 0.004 | - |
oleoyl-Ala-Ala-Pro-Val | - |
Homo sapiens | |
| 0.0058 | - |
oleoyl-Ala-Ala-Pro-Ala | - |
Homo sapiens | |
| 0.009 | - |
oleic acid | - |
Homo sapiens | |
| 0.025 | - |
CF3-CO-Ala-Ala-4-nitroanilide | - |
Homo sapiens | |
| 0.06 | - |
N-(1-(1-[1-(4-benzoyl-phenylcarbamoyl)-2-methyl-propylcarbamoyl]-3-methyl-butylcarbamoyl)-2-(4-hydroxy-phenyl)-ethyl)-succinamic acid | - |
Homo sapiens | |
| 0.12 | - |
succinyl-Tyr-D-Leu-D-Val-4-nitroanilide | - |
Homo sapiens | |
| 0.17 | - |
CF3-CO-Ala-Ala-Ala | - |
Homo sapiens | |
| 0.4 | - |
glutaryl-Ala-Ala-Pro-NH-C3H7 | - |
Homo sapiens | |
| 1.8 | - |
H-Ala-Ala-Pro-Ala-OH | - |
Homo sapiens | |
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Release 2023.1 (January 2023)
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