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Literature summary extracted from

  • Davies, L.C.; Friedlos, F.; Hedley, D.; Martin, J.; Ogilvie, L.M.; Scanlon, I.J.; Springer, C.J.
    Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy (2005), J. Med. Chem., 48, 5321-5328.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.17.11 drug development enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs Pseudomonas sp.
3.4.17.11 medicine enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs Pseudomonas sp.

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.17.11 (4-[bis(2-chloroethyl)amino]-2,3,5,6-tetrafluorobenzoyl)-L-glutamic acid prodrug, competitive inhibition Pseudomonas sp.
3.4.17.11 (4-[bis(2-iodoethyl)amino]-2,3,5,6-tetrafluorobenzoyl)-L-glutamic acid prodrug, competitive inhibition Pseudomonas sp.

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.17.11 0.0011
-
(4-[bis(2-bromoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0012
-
(4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0017
-
(4-[bis(2-chloroethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0017
-
(4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0026
-
(4-[bis(2-chloroethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0028
-
(4-[bis(2-iodoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 0.0034
-
(2-chloroethyl)-(2-(methylsulfoyloxyethyl)amino)aminobenzyl-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.17.11 Zn2+ required Pseudomonas sp.

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.17.11 (4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O Pseudomonas sp. a difluorinated prodrug 4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O Pseudomonas sp. RS16 a difluorinated prodrug 4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O Pseudomonas sp. a difluorinated prodrug 4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O Pseudomonas sp. RS16 a difluorinated prodrug 4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 additional information Pseudomonas sp. enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs, overview ?
-
?
3.4.17.11 additional information Pseudomonas sp. RS16 enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs, overview ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.4.17.11 Pseudomonas sp.
-
gene CPG2
-
3.4.17.11 Pseudomonas sp. RS16
-
gene CPG2
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.17.11 (2-chloroethyl)-(2-(methylsulfoyloxyethyl)amino)aminobenzyl-L-glutamic acid + H2O a prodrug Pseudomonas sp. (2-chloroethyl)-(2-(methylsulfoyloxyethyl)amino)aminobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-bromoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid + H2O a trifluorinated prodrug Pseudomonas sp. 4-[bis(2-bromoethyl)amino]-2,3,5-trifluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O a difluorinated prodrug Pseudomonas sp. 4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O a difluorinated prodrug Pseudomonas sp. RS16 4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-chloroethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid + H2O a trifluorinated prodrug Pseudomonas sp. 4-[bis(2-chloroethyl)amino]-2,3,5-trifluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-chloroethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O a difluorinated prodrug Pseudomonas sp. 4-[bis(2-chloroethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-iodoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid + H2O a trifluorinated prodrug Pseudomonas sp. 4-[bis(2-iodoethyl)amino]-2,3,5-trifluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O a difluorinated prodrug Pseudomonas sp. 4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 (4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid + H2O a difluorinated prodrug Pseudomonas sp. RS16 4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoic acid + L-glutamate
-
?
3.4.17.11 methotrexate + H2O
-
Pseudomonas sp. 4-[(2,4-diamino-6-(pteridinyl)methyl)-methylamino]-benzoic acid + L-glutamate
-
?
3.4.17.11 methotrexate + H2O
-
Pseudomonas sp. RS16 4-[(2,4-diamino-6-(pteridinyl)methyl)-methylamino]-benzoic acid + L-glutamate
-
?
3.4.17.11 additional information enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs, overview Pseudomonas sp. ?
-
?
3.4.17.11 additional information half-lives of prodrugs and drugs, overview Pseudomonas sp. ?
-
?
3.4.17.11 additional information enzyme is used in enzyme prodrug therapy to treat human breast cancer, the enzyme catalyzes the activation of the di- and trifluorinated prodrugs, overview Pseudomonas sp. RS16 ?
-
?
3.4.17.11 additional information half-lives of prodrugs and drugs, overview Pseudomonas sp. RS16 ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.17.11 carboxypeptidase G2
-
Pseudomonas sp.
3.4.17.11 CPG2
-
Pseudomonas sp.

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.17.11 37
-
assay at Pseudomonas sp.

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.17.11 220
-
(4-[bis(2-iodoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 583
-
(2-chloroethyl)-(2-(methylsulfoyloxyethyl)amino)aminobenzyl-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 732
-
(4-[bis(2-chloroethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 825
-
(4-[bis(2-bromoethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 827
-
(4-[bis(2-bromoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 1150
-
(4-[bis(2-iodoethyl)amino]-3,5-difluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.
3.4.17.11 1150
-
(4-[bis(2-chloroethyl)amino]-2,3,5-trifluorobenzoyl)-L-glutamic acid pH 7.3, 37 °C Pseudomonas sp.

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.17.11 7.3
-
assay at Pseudomonas sp.