Application | Comment | Organism |
---|---|---|
drug development | enediyne-amino acid conjugates as potent inhibitors of alpha-chymotrypsin | Bos taurus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-oxo-2-(1,2,7,8-tetradehydro-5,6-dihydro-4-benzazecin-4(3H)-yl)ethyl N-(tert-butoxycarbonyl)-L-phenylalaninate | enediyne-amino acid conjugate, competitive inhibitor | Bos taurus | |
2-oxo-2-(piperidin-1-yl)ethyl N-(tert-butoxycarbonyl)-L-phenylalaninate | piperidine amino acid conjugate, exhibits lesser inhibitory activity compared to the enediyne-peptide conjugates | Bos taurus | |
2-oxo-2-[(5Z)-3,4,7,8-tetradehydro-9,10-dihydroazecin-1(2H)-yl]ethyl N-(tert-butoxycarbonyl)-L-phenylalaninate | enediyne-amino acid conjugate | Bos taurus | |
4-[(4-nitrophenyl)sulfonyl]-1,2,7,8-tetradehydro-3,4,5,6-tetrahydro-4-benzazecine | - |
Bos taurus | |
additional information | novel synthesized enediyne-amino acid conjugates effectively target chymotrypsin inhibiting its proteolytic activity. Mode of inhibition is mostly competitive or of a mixed type depending on the nature of the inhibitor | Bos taurus | |
N-(tert-butoxycarbonyl)-L-alanyl-N-[4-[2-(3-oxoprop-1-yn-1-yl)phenyl]but-3-yn-1-yl]-L-phenylalaninamide | enediyne-amino acid conjugate | Bos taurus | |
tert-butyl [(2S)-1-(3,4-dihydroquinolin-1(2H)-yl)-1-oxo-3-phenylpropan-2-yl]carbamate | isoquinoline amino acid conjugate, exhibits lesser inhibitory activity compared to the enediyne-peptide conjugates, does not interact directly with the catalytic triad of chymotrypsin | Bos taurus | |
tert-butyl [(2S)-1-oxo-3-phenyl-1-(1,2,7,8-tetradehydro-5,6-dihydro-4-benzazecin-4(3H)-yl)propan-2-yl]carbamate | enediyne-amino acid conjugate | Bos taurus |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | required for catalysis | Bos taurus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | P00766 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
pancreas | - |
Bos taurus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Bovine serum albumin + H2O | - |
Bos taurus | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
alpha-chymotrypsin | - |
Bos taurus |
alpha-CT | - |
Bos taurus |
chymotrypsin | - |
Bos taurus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.003 | - |
tert-butyl [(2S)-1-oxo-3-phenyl-1-(1,2,7,8-tetradehydro-5,6-dihydro-4-benzazecin-4(3H)-yl)propan-2-yl]carbamate | in 80 mM Tris HCl buffer, pH 7.8 and 3 M CaCl2 | Bos taurus | |
0.012 | - |
N-(tert-butoxycarbonyl)-L-alanyl-N-[4-[2-(3-oxoprop-1-yn-1-yl)phenyl]but-3-yn-1-yl]-L-phenylalaninamide | in 80 mM Tris HCl buffer, pH 7.8 and 3 M CaCl2 | Bos taurus | |
0.03 | - |
2-oxo-2-(1,2,7,8-tetradehydro-5,6-dihydro-4-benzazecin-4(3H)-yl)ethyl N-(tert-butoxycarbonyl)-L-phenylalaninate | in 80 mM Tris HCl buffer, pH 7.8 and 3 M CaCl2 | Bos taurus | |
0.75 | - |
2-oxo-2-(piperidin-1-yl)ethyl N-(tert-butoxycarbonyl)-L-phenylalaninate | in 80 mM Tris HCl buffer, pH 7.8 and 3 M CaCl2 | Bos taurus |