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Literature summary extracted from
- Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the eta-carbonic anhydrase from Plasmodium falciparum (2016), Bioorg. Med. Chem. Lett., 26, 4184-4190 .
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 4.2.1.1 | cloning of the full domain of carbonic anhydrase from Plasmodium falciparum, which incorporates 358 amino acid residues, from 181 to 538, in the sequence of this 600 amino acid long protein, called PfCAdom | Plasmodium falciparum |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 4.2.1.1 | additional information | cloning of the full domain of carbonic anhydrase from Plasmodium falciparum, which incorporates 358 amino acid residues, from 181 to 538, in the sequence of this 600 amino acid long protein, called PfCAdom. PfCAdom is 13.3times more effective as a catalyst compared to the truncated form PfCA1. One of the highly conserved zinc coordinating histidines (His119 in hCA II) is not present in the truncated enzyme form PfCA1 since a Gln residue is found in the same, a tyrosine residue instead of a histidine is present in position 64 | Plasmodium falciparum |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 4.2.1.1 | (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~-thieno[3,2-e][1,2]thiazine-6-sulfonamide | - |
Plasmodium falciparum |  |
| 4.2.1.1 | (4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda~6~-thieno[2,3-b]thiopyran-2-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 1-(1,2-benzoxazol-3-yl)methanesulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 2-(hydroxymethyl)-4-nitro-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 2-methoxy-N-[(1-methylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 3,5-dichloro-2-hydroxybenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 3-aminobenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4,5-dichlorobenzene-1,3-disulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(1,1-dioxo-1lambda6,2-thiazinan-2-yl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(2-aminoethyl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(2-hydroxyethyl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(aminomethyl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-(hydroxymethyl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-3-bromobenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-3-chlorobenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-3-fluorobenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-6-chlorobenzene-1,3-disulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-N-(4-sulfamoylcyclopenta-1,3-dien-1-yl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-N-(4-sulfamoylphenyl)benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-N-[(4-sulfamoylphenyl)methyl]benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-aminobenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-hydroxybenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-methylbenzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-sulfamoylbenzoic acid | - |
Plasmodium falciparum | |
| 4.2.1.1 | 4-[(2-aminopyrimidin-4-yl)amino]benzene-1-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 5-amino-1,3,4-thiadiazole-2-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 5-[(benzenesulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1lambda6,2,4-benzothiadiazine-7-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~,2,4-benzothiadiazine-7-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | 6-ethoxy-1,3-benzothiazole-2-sulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | acetazolamide | 5-acetamido-1,3,4-thiadiazole-2-sulfonamide, AAZ | Plasmodium falciparum | |
| 4.2.1.1 | benzene-1,3-disulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | celecoxib | - |
Plasmodium falciparum | |
| 4.2.1.1 | methazolamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | additional information | sulfonamides CA inhibitors generally show much weaker inhibitory activity against PfCAdom compared to truncated PfCA | Plasmodium falciparum | |
| 4.2.1.1 | N~1~-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide | - |
Plasmodium falciparum | |
| 4.2.1.1 | [(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-2H,3aH,7H-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate | - |
Plasmodium falciparum | |
Metals/Ions
| EC Number | Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|---|
| 4.2.1.1 | additional information | homology modeling analysis shows that the metal ion coordination pattern of the eta-CA involves two His and one Gln residues in addition to the water molecule/hydroxide ion acting as nucleophile in the catalytic cycle | Plasmodium falciparum | |
| 4.2.1.1 | Zn2+ | required, metalloenzyme. The zinc ion is coordinated by residues His299, His301 and Gln320 | Plasmodium falciparum | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 4.2.1.1 | H2CO3 | Plasmodium falciparum | - |
CO2 + H2O | - |
r | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 4.2.1.1 | Plasmodium falciparum | Q8IHW5 | - |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 4.2.1.1 | CO2 + H2O | - |
Plasmodium falciparum | H2CO3 | - |
r | |
| 4.2.1.1 | H2CO3 | - |
Plasmodium falciparum | CO2 + H2O | - |
r | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 4.2.1.1 | eta-CA | - |
Plasmodium falciparum |
| 4.2.1.1 | PF3D7_1140000 | - |
Plasmodium falciparum |
| 4.2.1.1 | PfCAdom | - |
Plasmodium falciparum |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 4.2.1.1 | 22 | - |
assay at room temperature | Plasmodium falciparum |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 4.2.1.1 | 140000 | - |
CO2 | pH 7.5, 22°C, truncated form PfCA1, CO2 hydration reaction | Plasmodium falciparum | |
| 4.2.1.1 | 380000 | - |
CO2 | pH 7.5, 22°C, long enzyme form PfCAdom, CO2 hydration reaction | Plasmodium falciparum | |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 4.2.1.1 | 7.5 | - |
assay at | Plasmodium falciparum |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 4.2.1.1 | 0.000131 | - |
6-ethoxy-1,3-benzothiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA26 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000132 | - |
4-(1,1-dioxo-1lambda6,2-thiazinan-2-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA37 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000153 | - |
6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~,2,4-benzothiadiazine-7-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA38 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00017 | - |
acetazolamide | pH 7.5, 22°C, truncated form PfCA1, CO2 hydration reaction | Plasmodium falciparum | |
| 4.2.1.1 | 0.000198 | - |
methazolamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA25 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000217 | - |
celecoxib | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA36 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000226 | - |
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA35 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000246 | - |
1-(1,2-benzoxazol-3-yl)methanesulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA32 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00026 | - |
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~-thieno[3,2-e][1,2]thiazine-6-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA29 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000295 | - |
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-2H,3aH,7H-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA31 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000308 | - |
N~1~-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA34 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000366 | - |
acetazolamide | pH 7.5, 22°C, long enzyme form PfCAdom, CO2 hydration reaction | Plasmodium falciparum | |
| 4.2.1.1 | 0.000542 | - |
4,5-dichlorobenzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA27 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000581 | - |
3-aminobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA1 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000618 | - |
5-amino-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA13 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00063 | - |
3-aminobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000655 | - |
methazolamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000675 | - |
5-amino-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000704 | - |
4-(hydroxymethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA16 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000723 | - |
N~1~-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000726 | - |
4-(2-hydroxyethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA17 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000744 | - |
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA14 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00075 | - |
6-ethoxy-1,3-benzothiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000758 | - |
4-(2-aminoethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA6 | Plasmodium falciparum | |
| 4.2.1.1 | 0.000808 | - |
4-aminobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00089 | - |
4,5-dichlorobenzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000893 | - |
2-(hydroxymethyl)-4-nitro-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000904 | - |
4-(2-hydroxyethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000904 | - |
4-(aminomethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000912 | - |
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000957 | - |
3,5-dichloro-2-hydroxybenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.000963 | - |
(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda~6~-thieno[2,3-b]thiopyran-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA28 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00117 | - |
2-methoxy-N-[(1-methylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA33 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00133 | - |
5-[(benzenesulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA30 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0025 | - |
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00289 | - |
4-hydroxybenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00312 | - |
4-methylbenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00365 | - |
4-(aminomethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA5 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00414 | - |
4-amino-6-chlorobenzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA12 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00449 | - |
4-hydroxybenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA15 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00502 | - |
4-amino-3-bromobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00514 | - |
benzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00525 | - |
4-[(2-aminopyrimidin-4-yl)amino]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA19 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0054 | - |
4-amino-6-chlorobenzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00544 | - |
4-amino-3-bromobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA9 | Plasmodium falciparum | |
| 4.2.1.1 | 0.005545 | - |
4-amino-3-fluorobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA7 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00558 | - |
4-methylbenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA4 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0058 | - |
4-aminobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA2 | Plasmodium falciparum | |
| 4.2.1.1 | 0.005885 | - |
benzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA3 | Plasmodium falciparum | |
| 4.2.1.1 | 0.006175 | - |
4-amino-3-chlorobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA8 | Plasmodium falciparum | |
| 4.2.1.1 | 0.006225 | - |
4-[(2-aminopyrimidin-4-yl)amino]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0063 | - |
4-(hydroxymethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00631 | - |
3,5-dichloro-2-hydroxybenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA10 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0064 | - |
4-(2-aminoethyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.006705 | - |
4-amino-N-(4-sulfamoylcyclopenta-1,3-dien-1-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA20 | Plasmodium falciparum | |
| 4.2.1.1 | 0.00678 | - |
4-sulfamoylbenzoic acid | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA18 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0077 | - |
4-sulfamoylbenzoic acid | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.007835 | - |
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1lambda~6~-thieno[3,2-e][1,2]thiazine-6-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00789 | - |
1-(1,2-benzoxazol-3-yl)methanesulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00794 | - |
(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda~6~-thieno[2,3-b]thiopyran-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00814 | - |
4-amino-N-(4-sulfamoylphenyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00835 | - |
2-methoxy-N-[(1-methylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.00838 | - |
celecoxib | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0084 | - |
4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA24 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0102 | - |
4-amino-3-fluorobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0112 | - |
5-[(benzenesulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0113 | - |
4-amino-3-chlorobenzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0124 | - |
4-amino-N-(4-sulfamoylcyclopenta-1,3-dien-1-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.01245 | - |
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA11 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0128 | - |
2-(hydroxymethyl)-4-nitro-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA21 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0146 | - |
4-amino-N-[(4-sulfamoylphenyl)methyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA23 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0148 | - |
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-2H,3aH,7H-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.015 | - |
4-amino-N-(4-sulfamoylphenyl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCA22 | Plasmodium falciparum | |
| 4.2.1.1 | 0.0164 | - |
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0187 | - |
4-amino-N-[(4-sulfamoylphenyl)methyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0189 | - |
4-(1,1-dioxo-1lambda6,2-thiazinan-2-yl)benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0196 | - |
6-chloro-1,1-dioxo-1,2,3,4-tetrahydro-1lambda6,2,4-benzothiadiazine-7-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
| 4.2.1.1 | 0.0212 | - |
4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzene-1-sulfonamide | pH 7.5, 22°C, inhibition of CO2 hydration activity of PfCAdom | Plasmodium falciparum | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 4.2.1.1 | evolution | the enzyme belongs to the eta-CA class. Six genetically distinct CA families are known to date, the alpha-, beta-, gamma-, delta-, zeta- and eta-CAs. The alpha-, beta-, delta- and probably eta-CAs use Zn(II) ions at the active site, the gamma-CAs are probably Fe(II) enzymes, but they are active also with bound Zn(II) or Co(II) ions, whereas the zeta-class are cambialistic enzymes, active both with Cd(II) or Zn(II) bound within the active site | Plasmodium falciparum |
| 4.2.1.1 | additional information | the 69 amino acid residues insertion present in the active site of eta-CA PfCAdom seem to be crucial for the active site architecture | Plasmodium falciparum |
kcat/KM [mM/s]
| EC Number | kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 4.2.1.1 | 5400 | - |
CO2 | pH 7.5, 22°C, truncated form PfCA1, CO2 hydration reaction | Plasmodium falciparum | |
| 4.2.1.1 | 72000 | - |
CO2 | pH 7.5, 22°C, long enzyme form PfCAdom, CO2 hydration reaction | Plasmodium falciparum | |
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Release 2023.1 (January 2023)
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