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Literature summary for 3.4.17.11 extracted from

  • Masterson, L.A.; Spanswick, V.J.; Hartley, J.A.; Begent, R.H.; Howard, P.W.; Thurston, D.E.
    Synthesis and biological evaluation of novel pyrrolo[2,1-c][1,4]benzodiazepine prodrugs for use in antibody-directed enzyme prodrug therapy (2006), Bioorg. Med. Chem. Lett., 16, 252-256.
    View publication on PubMed

Application

Application Comment Organism
medicine the enzyme is used in antibody-directed enzyme prodrug therapy, ADEPT, e.g. against colorectal carcinoma expressing carcinoembryonic antigen, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information in vitro cytotoxicity of the prodrugs in LS174T colon cell line, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(2S,2'S)-2,2'-(pentane-1,5-diylbis[oxy[(11S,11aS)-11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8,10(5H)-diyl]carbonyloxymethanediylbenzene-4,1-diylcarbamoylimino])dipentanedioic acid + 2 H2O Homo sapiens
-
(11aS,11a'S)-8,8'-[pentane-1,5-diylbis(oxy)]bis(7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one) + ?
-
?
(2S,2'S)-2,2'-(pentane-1,5-diylbis[oxy[(11S,11aS)-11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8,10(5H)-diyl]carbonyloxymethanediylbenzene-4,1-diyloxycarbonylimino])dipentanedioic acid + 2 H2O Homo sapiens
-
3-hydroxybenzyl 4-hydroxybenzyl (11S,11aS,11'S,11a'S)-8,8'-[pentane-1,5-diylbis(oxy)]bis(11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-10(5H)-carboxylate) + 2 N-carboxy-L-glutamate
-
?
additional information Homo sapiens synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine prodrugs for use in antibody-directed enzyme prodrug therapy, overview ?
-
?
N-([4-[([[(11S,11aS)-11-hydroxy-7,8-dimethoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy)methyl]phenoxy]carbonyl)-L-glutamic acid + H2O Homo sapiens
-
(11aS)-7,8-dimethoxy-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one + ?
-
?
N-([4-[([[(11S,11aS)-11-hydroxy-7,8-dimethoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy)methyl]phenyl]carbamoyl)-L-glutamic acid + H2O Homo sapiens
-
? + L-glutamate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
LS174T cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(2S,2'S)-2,2'-(pentane-1,5-diylbis[oxy[(11S,11aS)-11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8,10(5H)-diyl]carbonyloxymethanediylbenzene-4,1-diylcarbamoylimino])dipentanedioic acid + 2 H2O
-
Homo sapiens (11aS,11a'S)-8,8'-[pentane-1,5-diylbis(oxy)]bis(7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one) + ?
-
?
(2S,2'S)-2,2'-(pentane-1,5-diylbis[oxy[(11S,11aS)-11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8,10(5H)-diyl]carbonyloxymethanediylbenzene-4,1-diyloxycarbonylimino])dipentanedioic acid + 2 H2O
-
Homo sapiens 3-hydroxybenzyl 4-hydroxybenzyl (11S,11aS,11'S,11a'S)-8,8'-[pentane-1,5-diylbis(oxy)]bis(11-hydroxy-7-methoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-10(5H)-carboxylate) + 2 N-carboxy-L-glutamate
-
?
additional information synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine prodrugs for use in antibody-directed enzyme prodrug therapy, overview Homo sapiens ?
-
?
N-([4-[([[(11S,11aS)-11-hydroxy-7,8-dimethoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy)methyl]phenoxy]carbonyl)-L-glutamic acid + H2O
-
Homo sapiens (11aS)-7,8-dimethoxy-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one + ?
-
?
N-([4-[([[(11S,11aS)-11-hydroxy-7,8-dimethoxy-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy)methyl]phenyl]carbamoyl)-L-glutamic acid + H2O
-
Homo sapiens ? + L-glutamate
-
?

Synonyms

Synonyms Comment Organism
carboxypeptidase G2
-
Homo sapiens
CPG2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens