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Literature summary for 2.5.1.58 extracted from

  • Eastman, R.T.; White, J.; Hucke, O.; Yokoyama, K.; Verlinde, C.L.; Hast, M.A.; Beese, L.S.; Gelb, M.H.; Rathod, P.K.; Van Voorhis, W.C.
    Resistance mutations at the lipid substrate binding site of Plasmodium falciparum protein farnesyltransferase (2007), Mol. Biochem. Parasitol., 152, 66-71.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.58

Protein Variants

Protein Variants Comment Organism
G612A decreased activity, mutant is resistant to the PFT inhibitors BMS-388891 and BMS-339941 Plasmodium falciparum
Y837C decreased activity, mutant is resistant to the PFT inhibitors BMS-388891 and BMS-339941 Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
BMS-339941
-
 Plasmodium falciparum
BMS-388891
-
 Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00002383
-
 farnesyl diphosphate wild type enzyme Plasmodium falciparum
0.0001275
-
 farnesyl diphosphate mutant enzyme Y837C Plasmodium falciparum
0.0002479
-
 farnesyl diphosphate mutant enzyme G612A Plasmodium falciparum
0.00032
-
 YRASNRSCAIM mutant enzyme Y837C Plasmodium falciparum
0.00064
-
 YRASNRSCAIM wild type enzyme Plasmodium falciparum
0.00303
-
 YRASNRSCAIM mutant enzyme G612A Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
ammonium sulfate fractionation and Q Sepharose chromatography Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine
-
 Plasmodium falciparum diphosphate + S-farnesyl protein
-
 ?
YRASNRSCAIM + farnesyl diphosphate
-
 Plasmodium falciparum YRASNRS-(S-farnesyl)CAIM + diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
PFT
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000022
-
 BMS-388891 wild type enzyme Plasmodium falciparum
0.0000009
-
 BMS-339941 wild type enzyme Plasmodium falciparum
0.0000012
-
 BMS-388891 mutant enzyme Y837C Plasmodium falciparum
0.0000028
-
 BMS-339941 mutant enzyme Y837C Plasmodium falciparum
0.0000112
-
 BMS-388891 mutant enzyme G612A Plasmodium falciparum
0.00003008
-
 BMS-339941 mutant enzyme G612A Plasmodium falciparum