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Literature summary extracted from

  • Dutta, S.; Basak, A.; Dasgupta, S.
    Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin (2009), Bioorg. Med. Chem., 17, 3900-3908.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.21.1 drug development enediyne-amino acid conjugates as potent inhibitors of alpha-chymotrypsin Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.1 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
3.4.21.1 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
3.4.21.1 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
3.4.21.1 4-[(4-nitrophenyl)sulfonyl]-1,2,7,8-tetradehydro-3,4,5,6-tetrahydro-4-benzazecine
-
 Bos taurus
3.4.21.1 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
3.4.21.1 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
3.4.21.1 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
3.4.21.1 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

EC Number Metals/Ions Comment Organism Structure
3.4.21.1 Ca2+ required for catalysis Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.1 Bos taurus P00766
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.1 pancreas
-
 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.1 Bovine serum albumin + H2O
-
 Bos taurus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.1 alpha-chymotrypsin
-
 Bos taurus
3.4.21.1 alpha-CT
-
 Bos taurus
3.4.21.1 chymotrypsin
-
 Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.1 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
3.4.21.1 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
3.4.21.1 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
3.4.21.1 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