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Literature summary for 3.5.3.1 extracted from

  • Hai, Y.; Christianson, D.
    Crystal structures of Leishmania mexicana arginase complexed with alpha,alpha-disubstituted boronic amino-acid inhibitors (2016), Acta Crystallogr. Sect. F, 72, 300-306 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.3.1

Application

Application Comment Organism
medicine Leishmania arginase is a potential drug target for the treatment of leishmaniasis because this binuclear manganese metalloenzyme initiates de novo polyamine biosynthesis by catalyzing the hydrolysis of L-arginine to generate L-ornithine and urea. The product L-ornithine subsequently undergoes decarboxylation to yield putrescine, which in turn is utilized for spermidine biosynthesis. Polyamines such as spermidine are essential for the growth and survival of the parasite, so inhibition of enzymes in the polyamine-biosynthetic pathway comprises an effective strategy for treating parasitic infections Leishmania mexicana

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallization by sitting-drop vapor diffusion method at 21°C. Crystal structures of the enzyme complexed with alpha,alpha-disubstituted boronic amino-acid inhibitors Leishmania mexicana

Inhibitors

Inhibitors Comment Organism Structure
(DL)-2-amino-6-borono-2-[1-(3,4-dichlorobenzyl)piperidin-4-yl]-hexanoic acid
-
 Leishmania mexicana
(R)-2-amino-6-borono-2-[1-(3,4-dichlorobenzyl)piperidin-4-yl]-hexanoic acid
-
 Leishmania mexicana
(R)-2-amino-6-borono-2-[2-(piperidin-1-yl)ethyl]hexanoic acid
-
 Leishmania mexicana
(S)-2-amino-6-borono-2-[2-(piperidin-1-yl)ethyl]hexanoic acid
-
 Leishmania mexicana
2-(S)-amino-6-boronohexanoic acid
-
 Leishmania mexicana

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ binuclear manganese metalloenzyme Leishmania mexicana

Organism

Organism UniProt Comment Textmining
Leishmania mexicana Q6TUJ5
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-arginine + H2O
-
 Leishmania mexicana L-ornithine + urea
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0009
-
 2-(S)-amino-6-boronohexanoic acid pH 8.0, 21°C Leishmania mexicana
0.0011
-
 (DL)-2-amino-6-borono-2-[1-(3,4-dichlorobenzyl)piperidin-4-yl]-hexanoic acid pH 8.0, 21°C Leishmania mexicana
0.0014
-
 (S)-2-amino-6-borono-2-[2-(piperidin-1-yl)ethyl]hexanoic acid pH 8.0, 21°C Leishmania mexicana

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0013
-
 pH 8.0, 21°C Leishmania mexicana 2-(S)-amino-6-boronohexanoic acid
0.0017
-
 pH 8.0, 21°C Leishmania mexicana (DL)-2-amino-6-borono-2-[1-(3,4-dichlorobenzyl)piperidin-4-yl]-hexanoic acid
0.0021
-
 pH 8.0, 21°C Leishmania mexicana (S)-2-amino-6-borono-2-[2-(piperidin-1-yl)ethyl]hexanoic acid

General Information

General Information Comment Organism
metabolism initiates de novo polyamine biosynthesis by catalyzing the hydrolysis of L-arginine to generate L-ornithine and urea. The product L-ornithine subsequently undergoes decarboxylation to yield putrescine, which in turn is utilized for spermidine biosynthesis Leishmania mexicana