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Literature summary for 1.3.1.9 extracted from

  • Tasdemir, D.; Lack, G.; Brun, R.; Rueedi, P.; Scapozza, L.; Perozzo, R.
    Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids (2006), J. Med. Chem., 49, 3345-3353.
    View publication on PubMed

Application

Application Comment Organism
medicine antimalarial target Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
for expression in Escherichia coli BL21DE3 CodonPlus-RIL cells Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(-)-catechin gallate IC50: 0.3 microM Plasmodium falciparum
(-)-epicatechin gallate IC50: 0.2 microM Plasmodium falciparum
(-)-epigallocatechin gallate IC 50: 0.2 microM Plasmodium falciparum
(-)-gallocatechin gallate IC50: 0.5 microM Plasmodium falciparum
3,7-dihydroxy-flavone IC50: 10 microM Plasmodium falciparum
acetoacetyl-CoA
-
Plasmodium falciparum
apigenin IC50: 50 microM Plasmodium falciparum
fisetin IC50: 1 microM Plasmodium falciparum
isorhamnetin IC50: 5 microM Plasmodium falciparum
kaempferol IC50: 20 microM Plasmodium falciparum
luteolin IC50: 2 microM Plasmodium falciparum
morin IC50: 5 microM Plasmodium falciparum
myricetin IC50: 0.4 microM Plasmodium falciparum
quercetin IC50: 1.5 microM Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acyl-[acyl-carrier protein] + NAD+ Plasmodium falciparum
-
trans-2,3-dehydroacyl-[acyl-carrier protein] + NADH + H+
-
?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using metal-chelate-affinity chromatography and gel filtration Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acyl-[acyl-carrier protein] + NAD+
-
Plasmodium falciparum trans-2,3-dehydroacyl-[acyl-carrier protein] + NADH + H+
-
?
crotonyl-CoA + NADH + H+ activity assay Plasmodium falciparum butyryl-CoA + NAD+
-
?

Synonyms

Synonyms Comment Organism
enoyl-[acyl-carrier-protein] reductase
-
Plasmodium falciparum
FabI
-
Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
activity assay Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
activity assay Plasmodium falciparum

Cofactor

Cofactor Comment Organism Structure
NADH
-
Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00004
-
acetoacetyl-CoA (-)-catechin gallate Plasmodium falciparum
0.0021
-
acetoacetyl-CoA luteolin Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0002
-
IC 50: 0.2 microM Plasmodium falciparum (-)-epigallocatechin gallate
0.0002
-
IC50: 0.2 microM Plasmodium falciparum (-)-epicatechin gallate
0.0003
-
IC50: 0.3 microM Plasmodium falciparum (-)-catechin gallate
0.0004
-
IC50: 0.4 microM Plasmodium falciparum myricetin
0.0005
-
IC50: 0.5 microM Plasmodium falciparum (-)-gallocatechin gallate
0.001
-
IC50: 1 microM Plasmodium falciparum fisetin
0.0015
-
IC50: 1.5 microM Plasmodium falciparum quercetin
0.002
-
IC50: 2 microM Plasmodium falciparum luteolin
0.005
-
IC50: 5 microM Plasmodium falciparum morin
0.005
-
IC50: 5 microM Plasmodium falciparum isorhamnetin
0.01
-
IC50: 10 microM Plasmodium falciparum 3,7-dihydroxy-flavone
0.02
-
IC50: 20 microM Plasmodium falciparum kaempferol
0.05
-
IC50: 50 microM Plasmodium falciparum apigenin