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Literature summary 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

EC Number Application Comment Organism
1.3.1.9 medicine antimalarial target Plasmodium falciparum

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.9 (-)-catechin gallate IC50: 0.3 microM Plasmodium falciparum
1.3.1.9 (-)-epicatechin gallate IC50: 0.2 microM Plasmodium falciparum
1.3.1.9 (-)-epigallocatechin gallate IC 50: 0.2 microM Plasmodium falciparum
1.3.1.9 (-)-gallocatechin gallate IC50: 0.5 microM Plasmodium falciparum
1.3.1.9 3,7-dihydroxy-flavone IC50: 10 microM Plasmodium falciparum
1.3.1.9 acetoacetyl-CoA
-
 Plasmodium falciparum
1.3.1.9 apigenin IC50: 50 microM Plasmodium falciparum
1.3.1.9 fisetin IC50: 1 microM Plasmodium falciparum
1.3.1.9 isorhamnetin IC50: 5 microM Plasmodium falciparum
1.3.1.9 kaempferol IC50: 20 microM Plasmodium falciparum
1.3.1.9 luteolin IC50: 2 microM Plasmodium falciparum
1.3.1.9 morin IC50: 5 microM Plasmodium falciparum
1.3.1.9 myricetin IC50: 0.4 microM Plasmodium falciparum
1.3.1.9 quercetin IC50: 1.5 microM Plasmodium falciparum

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.9 Plasmodium falciparum
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.3.1.9 25
-
 activity assay Plasmodium falciparum

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.3.1.9 7.4
-
 activity assay Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.1.9 NADH
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.3.1.9 0.00004
-
 acetoacetyl-CoA (-)-catechin gallate Plasmodium falciparum
1.3.1.9 0.0021
-
 acetoacetyl-CoA luteolin Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.1.9 0.0002
-
 IC 50: 0.2 microM Plasmodium falciparum (-)-epigallocatechin gallate
1.3.1.9 0.0002
-
 IC50: 0.2 microM Plasmodium falciparum (-)-epicatechin gallate
1.3.1.9 0.0003
-
 IC50: 0.3 microM Plasmodium falciparum (-)-catechin gallate
1.3.1.9 0.0004
-
 IC50: 0.4 microM Plasmodium falciparum myricetin
1.3.1.9 0.0005
-
 IC50: 0.5 microM Plasmodium falciparum (-)-gallocatechin gallate
1.3.1.9 0.001
-
 IC50: 1 microM Plasmodium falciparum fisetin
1.3.1.9 0.0015
-
 IC50: 1.5 microM Plasmodium falciparum quercetin
1.3.1.9 0.002
-
 IC50: 2 microM Plasmodium falciparum luteolin
1.3.1.9 0.005
-
 IC50: 5 microM Plasmodium falciparum morin
1.3.1.9 0.005
-
 IC50: 5 microM Plasmodium falciparum isorhamnetin
1.3.1.9 0.01
-
 IC50: 10 microM Plasmodium falciparum 3,7-dihydroxy-flavone
1.3.1.9 0.02
-
 IC50: 20 microM Plasmodium falciparum kaempferol
1.3.1.9 0.05
-
 IC50: 50 microM Plasmodium falciparum apigenin