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Literature summary for 2.7.1.227 extracted from

  • Mina, J.G.; Mosely, J.A.; Ali, H.Z.; Denny, P.W.; Steel, P.G.
    Exploring Leishmania major inositol phosphorylceramide synthase (LmjIPCS) insights into the ceramide binding domain (2011), Org. Biomol. Chem., 9, 1823-1830 .
    View publication on PubMed
Search for more literature for 2.7.1.227

Inhibitors

Inhibitors Comment Organism Structure
(2R,4E)-2-aminooctadec-4-en-1-ol compound displays significant anti-protozoal effects at the concentrations analyzed Leishmania major
additional information synthesis of ceramide derivatives built around a set of hydroxybutenyl amine cores, exploring variations in the sphingosine tail, N-acyl unit and the degree of hydroxylation. The N-acyl chain contributes to affinity, analogues lacking the amide linkage function as competitive inhibitors in both enzyme and cell-based assays Leishmania major
N-[(2R,4E)-1-hydroxyoctadec-4-en-2-yl]-2-phenylacetamide
-
 Leishmania major
N-[(2S,4E)-3-hydroxyoctadec-4-en-2-yl]octanamide
-
 Leishmania major

Organism

Organism UniProt Comment Textmining
Leishmania major E9AFX2
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-phosphatidyl-1D-myo-inositol + N-[(2R,4E)-1-hydroxyoctadec-4-en-2-yl]octanamide
-
 Leishmania major 1,2-diacyl-sn-glycerol + ?
-
 ?
additional information synthesis of ceramide derivatives built around a set of hydroxybutenyl amine cores, exploring variations in the sphingosine tail, N-acyl unit and the degree of hydroxylation. The C-3 hydroxyl group is not essential for turnover but it provides enhanced affinity. A long (C13) hydrocarbon ceramide tail is necessary for both high affinity and turnover. The N-acyl chain also contributes to affinity, analogues lacking the amide linkage function as competitive inhibitors in both enzyme and cell-based assays Leishmania major ?
-
 ?

Synonyms

Synonyms Comment Organism
IPCS
-
 Leishmania major
LMJF_35_4990
-
 Leishmania major
phosphatidylinositol:ceramide inositolphosphotransferase
-
 Leishmania major

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0048
-
 pH not specified in the publication, temperature not specified in the publication Leishmania major N-[(2S,4E)-3-hydroxyoctadec-4-en-2-yl]octanamide
0.0132
-
 pH not specified in the publication, temperature not specified in the publication Leishmania major N-[(2R,4E)-1-hydroxyoctadec-4-en-2-yl]-2-phenylacetamide
0.0147
-
 pH not specified in the publication, temperature not specified in the publication Leishmania major (2R,4E)-2-aminooctadec-4-en-1-ol