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Literature summary for 2.5.1.15 extracted from

  • Pornthanakasem, W.; Riangrungroj, P.; Chitnumsub, P.; Ittarat, W.; Kongkasuriyachai, D.; Uthaipibull, C.; Yuthavong, Y.; Leartsakulpanich, U.
    Role of Plasmodium vivax dihydropteroate synthase polymorphisms in sulfa drug resistance (2016), Antimicrob. Agents Chemother., 60, 4453-4463 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.15

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Rosetta(DE3)pLysS Plasmodium vivax

Protein Variants

Protein Variants Comment Organism
A383G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
A383G/A553G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
S382A/A383G/A553G mutation does not much influence the enzyme catalytic activity. Mutant becomes 13fold more resistant to sulfadoxine than the wild type Plasmodium vivax
V585A 2fold increase in the level of resistance to sulfadoxine compared with that of the wild type carrying V585A. V585A mutant is 4fold more resistant to dapsone than the wild type Plasmodium vivax

Inhibitors

Inhibitors Comment Organism Structure
dapsone
-
 Plasmodium vivax
sulfadoxine
-
 Plasmodium vivax
sulfathiazole
-
 Plasmodium vivax

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00015
-
 4-Aminobenzoate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.00019
-
 4-Aminobenzoate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.00026
-
 4-Aminobenzoate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.00033
-
 4-Aminobenzoate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.00048
-
 4-Aminobenzoate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
174000
-
 gel filtration Plasmodium vivax

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate Plasmodium vivax
-
 diphosphate + 7,8-dihydropteroate
-
 ?

Organism

Organism UniProt Comment Textmining
Plasmodium vivax
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Plasmodium vivax

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate
-
 Plasmodium vivax diphosphate + 7,8-dihydropteroate
-
 ?

Subunits

Subunits Comment Organism
homodimer 2 * 85000, SDS-PAGE Plasmodium vivax

Synonyms

Synonyms Comment Organism
DHPS-HPPK bifunctional enzyme Plasmodium vivax
dihydropteroate synthase/hydroxymethyldihydropterin pyrophosphokinase bifunctional enzyme Plasmodium vivax

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0024
-
 4-Aminobenzoate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.0024
-
 (7,8-dihydropterin-6-yl)methyl diphosphate wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.0029
-
 4-Aminobenzoate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.0029
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.0055
-
 4-Aminobenzoate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.0055
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.006
-
 4-Aminobenzoate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.006
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.0134
-
 4-Aminobenzoate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.0134
-
 (7,8-dihydropterin-6-yl)methyl diphosphate mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00011
-
 dapsone wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.00015
-
 sulfathiazole wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.00019
-
 sulfathiazole mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.00053
-
 dapsone mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.0015
-
 sulfadoxine wild-type enzyme, pH 9.0, 37°C Plasmodium vivax
0.00295
-
 sulfathiazole mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.003
-
 sulfadoxine mutant enzyme V585A, pH 9.0, 37°C Plasmodium vivax
0.00367
-
 dapsone mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.00454
-
 dapsone mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.01553
-
 sulfathiazole mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.01773
-
 dapsone mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.019
-
 sulfathiazole mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.0481
-
 sulfadoxine mutant enzyme A383G, pH 9.0, 37°C Plasmodium vivax
0.176
-
 sulfadoxine mutant enzyme A383G/A553G, pH 9.0, 37°C Plasmodium vivax
0.227
-
 sulfadoxine mutant enzyme S382A/A383G/A553G, pH 9.0, 37°C Plasmodium vivax

General Information

General Information Comment Organism
drug target the enzyme is a sulfa drug target in malaria treatment Plasmodium vivax