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Literature summary for 4.1.1.17 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
Search for more literature for 4.1.1.17

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei P07805
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
ODC
-
 Trypanosoma brucei

Turnover Number [1/s]

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

Cofactor

Cofactor Comment Organism Structure
pyridoxal 5'-phosphate
-
 Trypanosoma brucei

Ki Value [mM]

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

IC50 Value

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

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