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Literature summary for 2.7.1.33 extracted from

  • Spry, C.; Chai, C.L.; Kirk, K.; Saliba, K.J.
    A class of pantothenic acid analogs inhibits Plasmodium falciparum pantothenate kinase and represses the proliferation of malaria parasites (2005), Antimicrob. Agents Chemother., 49, 4649-4657.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.33

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2,4-dihydroxy-3,3-dimethyl-N'-phenylbutanohydrazide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Homo sapiens
(2R)-2,4-dihydroxy-3,3-dimethyl-N'-phenylbutanohydrazide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
(2R)-2,4-dihydroxy-3,3-dimethylbutanohydrazide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
(2R)-2,4-dihydroxy-N-(2-hydroxyethyl)-3,3-dimethylbutanamide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
(2R)-N-(2,3-dihydroxypropyl)-2,4-dihydroxy-3,3-dimethylbutanamide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
(2R)-N-allyl-2,4-dihydroxy-3,3-dimethylbutanamide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Homo sapiens
(2R)-N-allyl-2,4-dihydroxy-3,3-dimethylbutanamide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
2,4-dihydroxy-3,3-dimethyl N-(2-pentylcarbamoyl-ethyl)-butyramide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
2,4-dihydroxy-3,3-dimethyl N-(2-propylcarbamoylethyl)-butyramide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
2,4-dihydroxy-3,3-dimethyl N-[2-(3-ethoxy-propylcarbamoyl)-ethyl]-butyramide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
2,4-dihydroxy-3,3-dimethyl N-[2-(3-methylsulfanylpropylcarbamoyl)-ethyl]-butyramide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
2,4-dihydroxy-N-[2-(3-methoxy-propylcarbamoyl)-ethyl]-3,3-dimethyl-butyramide competitive, pantothenic acid analogue with 2,4-dihydroxy-3,3-dimethylbutyramide core of pantothenate, inhibition mechanism Plasmodium falciparum
additional information in vivo antiplasmodial activities of the inhibitor molecules, overview Plasmodium falciparum
pantothenol competitive inhibition Plasmodium falciparum

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens
Mg2+
-
 Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + (R)-pantothenate Homo sapiens first step in coenzyme A biosynthesis ADP + (R)-4'-phosphopantothenate
-
 ?
ATP + (R)-pantothenate Plasmodium falciparum first step in coenzyme A biosynthesis ADP + (R)-4'-phosphopantothenate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
JURKAT cell
-
 Homo sapiens
-
trophozoite
-
 Plasmodium falciparum
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + (R)-pantothenate
-
 Homo sapiens ADP + (R)-4'-phosphopantothenate
-
 ?
ATP + (R)-pantothenate
-
 Plasmodium falciparum ADP + (R)-4'-phosphopantothenate
-
 ?
ATP + (R)-pantothenate first step in coenzyme A biosynthesis Homo sapiens ADP + (R)-4'-phosphopantothenate
-
 ?
ATP + (R)-pantothenate first step in coenzyme A biosynthesis Plasmodium falciparum ADP + (R)-4'-phosphopantothenate
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens
37
-
 assay at Plasmodium falciparum

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens
ATP
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0019
-
 (2R)-2,4-dihydroxy-N-(2-hydroxyethyl)-3,3-dimethylbutanamide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.013
-
 (2R)-2,4-dihydroxy-3,3-dimethylbutanohydrazide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.076
-
 2,4-dihydroxy-3,3-dimethyl N-[2-(3-methylsulfanylpropylcarbamoyl)-ethyl]-butyramide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.082
-
 (2R)-N-allyl-2,4-dihydroxy-3,3-dimethylbutanamide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.109
-
 2,4-dihydroxy-N-[2-(3-methoxy-propylcarbamoyl)-ethyl]-3,3-dimethyl-butyramide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.111
-
 2,4-dihydroxy-3,3-dimethyl N-[2-(3-ethoxy-propylcarbamoyl)-ethyl]-butyramide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.112
-
 2,4-dihydroxy-3,3-dimethyl N-(2-propylcarbamoylethyl)-butyramide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.129
-
 pantothenol 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.138
-
 (2R)-2,4-dihydroxy-3,3-dimethyl-N'-phenylbutanohydrazide 37°C, versus pantothenate at 1 mM Homo sapiens
0.162
-
 2,4-dihydroxy-3,3-dimethyl N-(2-pentylcarbamoyl-ethyl)-butyramide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
0.2
-
 (2R)-2,4-dihydroxy-3,3-dimethyl-N'-phenylbutanohydrazide 37°C, versus pantothenate at 1 mM Plasmodium falciparum
1
-
 (2R)-N-allyl-2,4-dihydroxy-3,3-dimethylbutanamide 37°C, versus pantothenate at 1 mM Homo sapiens
4
-
 (2R)-N-(2,3-dihydroxypropyl)-2,4-dihydroxy-3,3-dimethylbutanamide 37°C, versus pantothenate at 1 mM Plasmodium falciparum