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Literature summary extracted from

  • Smithson, D.C.; Lee, J.; Shelat, A.A.; Phillips, M.A.; Guy, R.K.
    Discovery of potent and selective inhibitors of Trypanosoma brucei ornithine decarboxylase (2010), J. Biol. Chem., 285, 16771-16781.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
4.1.1.17 expressed in Escherichia coli BL21(DE3) cells Trypanosoma brucei

Protein Variants

EC Number Protein Variants Comment Organism
4.1.1.17 D364E the mutant shows almost no activity compared to the wild type enzyme Trypanosoma brucei
4.1.1.17 S396A the mutant shows about 2fold increased activity compared to the wild type enzyme Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.1.1.17 1H-indol-3-yl(morpholin-4-yl)acetonitrile
-
 Trypanosoma brucei
4.1.1.17 2-phenylethyl carbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 3-(morpholin-4-ylmethyl)-1H-indole
-
 Trypanosoma brucei
4.1.1.17 4,4'-[pentane-1,5-diylbis(oxy)]dibenzenecarboximidamide
-
 Trypanosoma brucei
4.1.1.17 alexidine
-
 Trypanosoma brucei
4.1.1.17 benzene-1,3-diyldiethane-2,1-diyl dicarbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 benzene-1,4-diyldimethanediyl dicarbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 but-2-yne-1,4-diyl dicarbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 butane-1,4-diyl dicarbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzamide
-
 Trypanosoma brucei
4.1.1.17 N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide
-
 Trypanosoma brucei
4.1.1.17 N-(4-ethoxy-1,3-benzothiazol-2-yl)benzamide
-
 Trypanosoma brucei
4.1.1.17 N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide
-
 Trypanosoma brucei
4.1.1.17 pentane-1,5-diyl dicarbamimidothioate
-
 Trypanosoma brucei
4.1.1.17 propane-1,3-diyl dicarbamimidothioate
-
 Trypanosoma brucei

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
4.1.1.17 0.27
-
 L-ornithine mutant enzyme S396A, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.37
-
 L-ornithine wild type enzyme, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 55.2
-
 L-ornithine mutant enzyme D364E, at pH 7.5 and 37°C Trypanosoma brucei

Organism

EC Number Organism UniProt Comment Textmining
4.1.1.17 Trypanosoma brucei P07805
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
4.1.1.17 Ni2+-NTA-agarose column chromatography and Superdex 200 gel filtration Trypanosoma brucei

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.1.1.17 L-ornithine
-
 Trypanosoma brucei putrescine + CO2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
4.1.1.17 ODC
-
 Trypanosoma brucei

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
4.1.1.17 0.015
-
 L-ornithine mutant enzyme D364E, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 7
-
 L-ornithine wild type enzyme, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 10
-
 L-ornithine mutant enzyme S396A, at pH 7.5 and 37°C Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
4.1.1.17 pyridoxal 5'-phosphate
-
 Trypanosoma brucei

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.1.1.17 0.0027
-
 alexidine at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.0036
-
 benzene-1,3-diyldiethane-2,1-diyl dicarbamimidothioate at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.0102
-
 pentane-1,5-diyl dicarbamimidothioate at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.014
-
 N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.0271
-
 1H-indol-3-yl(morpholin-4-yl)acetonitrile at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.0288
-
 butane-1,4-diyl dicarbamimidothioate at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.0289
-
 4,4'-[pentane-1,5-diylbis(oxy)]dibenzenecarboximidamide at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 N-(4-ethoxy-1,3-benzothiazol-2-yl)benzamide Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzamide Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 but-2-yne-1,4-diyl dicarbamimidothioate Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 propane-1,3-diyl dicarbamimidothioate Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 2-phenylethyl carbamimidothioate Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 3-(morpholin-4-ylmethyl)-1H-indole Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 0.1
-
 benzene-1,4-diyldimethanediyl dicarbamimidothioate Ki above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
4.1.1.17 0.014
-
 at pH 7.5 and 37°C Trypanosoma brucei benzene-1,3-diyldiethane-2,1-diyl dicarbamimidothioate
4.1.1.17 0.0153
-
 at pH 7.5 and 37°C Trypanosoma brucei pentane-1,5-diyl dicarbamimidothioate
4.1.1.17 0.02
-
 at pH 7.5 and 37°C Trypanosoma brucei 1H-indol-3-yl(morpholin-4-yl)acetonitrile
4.1.1.17 0.024
-
 at pH 7.5 and 37°C Trypanosoma brucei alexidine
4.1.1.17 0.0303
-
 at pH 7.5 and 37°C Trypanosoma brucei butane-1,4-diyl dicarbamimidothioate
4.1.1.17 0.0342
-
 at pH 7.5 and 37°C Trypanosoma brucei 4,4'-[pentane-1,5-diylbis(oxy)]dibenzenecarboximidamide
4.1.1.17 0.0594
-
 at pH 7.5 and 37°C Trypanosoma brucei N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide
4.1.1.17 0.075
-
 at pH 7.5 and 37°C Trypanosoma brucei propane-1,3-diyl dicarbamimidothioate
4.1.1.17 0.075
-
 at pH 7.5 and 37°C Trypanosoma brucei benzene-1,4-diyldimethanediyl dicarbamimidothioate
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-propoxybenzamide
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei N-(4-ethoxy-1,3-benzothiazol-2-yl)benzamide
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei N-(4-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzamide
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei but-2-yne-1,4-diyl dicarbamimidothioate
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei 2-phenylethyl carbamimidothioate
4.1.1.17 0.1
-
 IC50 above 0.1 mM, at pH 7.5 and 37°C Trypanosoma brucei 3-(morpholin-4-ylmethyl)-1H-indole

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
4.1.1.17 0.00027
-
 L-ornithine mutant enzyme D364E, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 18.9
-
 L-ornithine wild type enzyme, at pH 7.5 and 37°C Trypanosoma brucei
4.1.1.17 37
-
 L-ornithine mutant enzyme S396A, at pH 7.5 and 37°C Trypanosoma brucei