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Literature summary for 2.7.7.13 extracted from

  • Pomel, S.; Mao, W.; Ha-Duong, T.; Cave, C.; Loiseau, P.
    GDP-mannose pyrophosphorylase A biologically validated target for drug development against leishmaniasis (2019), Front. Cell. Infect. Microbiol., 9, 186 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline competitive inhibitor Homo sapiens
4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline competitive inhibitor Leishmania donovani
4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline competitive inhibitor Leishmania mexicana
miltefosine
-
Leishmania donovani
miltefosine
-
Leishmania mexicana
tetrapropan-2-yl [5-(1-[2-[(quinolin-2-yl)methoxy]ethyl]-1H-1,2,3-triazol-4-yl)pent-1-yne-4,4-diyl]bis(phosphonate) competitive inhibitor Leishmania donovani
tetrapropan-2-yl [5-(1-[2-[(quinolin-2-yl)methoxy]ethyl]-1H-1,2,3-triazol-4-yl)pent-1-yne-4,4-diyl]bis(phosphonate) competitive inhibitor Leishmania mexicana

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-
cytosol
-
Leishmania donovani 5829
-
cytosol
-
Leishmania mexicana 5829
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens
Mg2+ required Leishmania donovani
Mg2+ required Leishmania mexicana

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP + alpha-D-mannose 1-phosphate Homo sapiens
-
diphosphate + GDP-mannose
-
r
GTP + alpha-D-mannose 1-phosphate Leishmania donovani
-
diphosphate + GDP-mannose
-
r
GTP + alpha-D-mannose 1-phosphate Leishmania mexicana
-
diphosphate + GDP-mannose
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Leishmania donovani
-
-
-
Leishmania mexicana
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
Leishmania donovani
-
amastigote
-
Leishmania mexicana
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + alpha-D-mannose 1-phosphate
-
Homo sapiens diphosphate + GDP-mannose
-
r
GTP + alpha-D-mannose 1-phosphate
-
Leishmania donovani diphosphate + GDP-mannose
-
r
GTP + alpha-D-mannose 1-phosphate
-
Leishmania mexicana diphosphate + GDP-mannose
-
r

Subunits

Subunits Comment Organism
hexamer
-
Homo sapiens
hexamer
-
Leishmania donovani
hexamer
-
Leishmania mexicana

Synonyms

Synonyms Comment Organism
GDP-mannose pyrophosphorylase
-
Homo sapiens
GDP-mannose pyrophosphorylase
-
Leishmania donovani
GDP-mannose pyrophosphorylase
-
Leishmania mexicana
GDP-MP
-
Homo sapiens
GDP-MP
-
Leishmania donovani
GDP-MP
-
Leishmania mexicana

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00106
-
pH and temperature not specified in the publication Leishmania donovani tetrapropan-2-yl [5-(1-[2-[(quinolin-2-yl)methoxy]ethyl]-1H-1,2,3-triazol-4-yl)pent-1-yne-4,4-diyl]bis(phosphonate)
0.00208
-
pH and temperature not specified in the publication Leishmania donovani miltefosine
0.02
-
pH and temperature not specified in the publication Homo sapiens 4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline
0.02374
-
pH and temperature not specified in the publication Leishmania mexicana miltefosine
0.03068
-
pH and temperature not specified in the publication Leishmania donovani 4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline
0.04925
-
pH and temperature not specified in the publication Leishmania mexicana 4-[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]-7-chloroquinoline
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Leishmania mexicana tetrapropan-2-yl [5-(1-[2-[(quinolin-2-yl)methoxy]ethyl]-1H-1,2,3-triazol-4-yl)pent-1-yne-4,4-diyl]bis(phosphonate)