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Literature summary for 2.7.7.13 extracted from

  • Lackovic, K.; Parisot, J.P.; Sleebs, N.; Baell, J.B.; Debien, L.; Watson, K.G.; Curtis, J.M.; Handman, E.; Street, I.P.; Kedzierski, L.
    Inhibitors of Leishmania GDP-mannose pyrophosphorylase identified by high-throughput screening of small-molecule chemical library (2010), Antimicrob. Agents Chemother., 54, 1712-1719.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression of His6-tagged enzyme in Escherichia coli strain BL21(DE3)pLysS Leishmania major

Inhibitors

Inhibitors Comment Organism Structure
(4E)-4-[(6-chloro-1,3-benzodioxol-5-yl)methylidene]-1-(3,4-dimethylphenyl)pyrazolidine-3,5-dione
-
Leishmania major
(4Z)-1-(4-fluorophenyl)-4-[(5-methyltetrahydrofuran-2-yl)methylidene]pyrazolidine-3,5-dione
-
Leishmania major
2-(5-ethyl-1,3,4-thiadiazol-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione
-
Leishmania major
2-methyl-9H-pyrido[2,3-b]indole
-
Leishmania major
3-(2,3-dihydroimidazo[2,1-b][1,3]thiazol-5-yl)-1H-indole
-
Leishmania major
3-(2-ethyl-5-methyl-2H-pyrrol-3-yl)-6-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
3-[2-(4-methoxyphenyl)ethyl]-2H-1,2,4-benzothiadiazine 1,1-dioxide
-
Leishmania major
4-(4-benzylpiperazin-1-yl)-7-chloroquinoline
-
Leishmania major
4-[4-(4-tert-butylbenzyl)piperazin-1-yl]-7-chloroquinoline
-
Leishmania major
4-[4-(biphenyl-4-ylmethyl)piperazin-1-yl]-7-chloroquinoline
-
Leishmania major
5-methyl-2-(2-phenylethyl)-1H-benzimidazole
-
Leishmania major
6-(1-ethyl-3-propyl-1H-pyrazol-5-yl)-3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-(2,4-dichlorophenyl)-3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-(2-chloro-6-fluorobenzyl)-3-(2-ethyl-5-methyl-2H-pyrrol-3-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-(2-chloro-6-fluorobenzyl)-3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-(4-chlorophenyl)-3-(2-methylbenzyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-(4-fluorophenyl)-3-(4-methoxyphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
6-[[(4,6-dimethylpyrimidin-2-yl)sulfanyl]methyl]-3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
-
Leishmania major
7-chloro-4-(4-methylpiperazin-1-yl)quinoline
-
Leishmania major
7-methoxy-4-oxo-4H-thiochromene-3-carboxylic acid
-
Leishmania major
8-(dimethylamino)-7-hydroxy-3-(1-phenyl-1H-pyrazol-4-yl)-4H-chromen-4-one
-
Leishmania major
9-(3,4-dimethoxyphenyl)-2,3-dihydroimidazo[1,2-c]thieno[3,2-e]pyrimidine
-
Leishmania major
ethyl (2Z)-(hydroxyimino)(1H-tetrazol-5-yl)ethanoate
-
Leishmania major
methyl 1-cyano-2-hydroxy-9,10-dimethoxy-4-oxo-6,7-dihydro-4H-pyrido[2,1-a]isoquinoline-3-carboxylate
-
Leishmania major
additional information high-throughput GDP-MP inhibitor large-scale screening, overview Leishmania major
[4-(7-chloroquinolin-4-yl)piperazin-1-yl](4-methylphenyl)methanone
-
Leishmania major

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP + alpha-D-mannose 1-phosphate Leishmania major
-
diphosphate + GDP-mannose
-
?

Organism

Organism UniProt Comment Textmining
Leishmania major
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His6-tagged enzyme from Escherichia coli strain BL21(DE3)pLysS by metal affinity chromatograhy Leishmania major

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
Leishmania major
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + alpha-D-mannose 1-phosphate
-
Leishmania major diphosphate + GDP-mannose
-
?
additional information GDP-MP high-throughput screening assay method devlopment and evaluation, overview Leishmania major ?
-
?

Synonyms

Synonyms Comment Organism
GDP-mannose pyrophosphorylase
-
Leishmania major
GDP-MP
-
Leishmania major

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Leishmania major