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Literature summary extracted from

  • Minakuchi, T.; Nishimori, I.; Vullo, D.; Scozzafava, A.; Supuran, C.T.
    Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate (2009), J. Med. Chem., 52, 2226-2232.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
4.2.1.1 expressed in Escherichia coli BL21(DE3) cells Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.2.1.1 2-aminobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 3-(4-sulfamoylphenyl)propanoic acid
-
 Mycobacterium tuberculosis
4.2.1.1 3-bromosulfanilamide
-
 Mycobacterium tuberculosis
4.2.1.1 4,5-dichloro-benzene-1,3-disulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-(2-aminoethyl)benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-(2-hydroxyethyl)benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-(aminomethyl)benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-(hydroxymethyl)benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-3-bromobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-3-chlorobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-3-fluorobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-3-iodobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-6-chlorobenzene-1,3-disulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-Aminobenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-methylbenzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 4-sulfamoylbenzoic acid
-
 Mycobacterium tuberculosis
4.2.1.1 4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 5-amino-1,3,4-thiadiazole-2-sulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 5-[[(4-aminophenyl)sulfonyl]amino]-1,3,4-thiadiazole-2-sulfonamide
-
 Mycobacterium tuberculosis
4.2.1.1 acetazolamide
-
 Mycobacterium tuberculosis
4.2.1.1 benzolamide
-
 Mycobacterium tuberculosis
4.2.1.1 brinzolamide
-
 Mycobacterium tuberculosis
4.2.1.1 celecoxib
-
 Mycobacterium tuberculosis
4.2.1.1 dorzolamide
-
 Mycobacterium tuberculosis
4.2.1.1 ethoxzolamide
-
 Mycobacterium tuberculosis
4.2.1.1 indisulam
-
 Mycobacterium tuberculosis
4.2.1.1 methazolamide
-
 Mycobacterium tuberculosis
4.2.1.1 saccharin
-
 Mycobacterium tuberculosis
4.2.1.1 sulpiride
-
 Mycobacterium tuberculosis
4.2.1.1 sulthiame
-
 Mycobacterium tuberculosis
4.2.1.1 topiramate
-
 Mycobacterium tuberculosis
4.2.1.1 valdecoxib
-
 Mycobacterium tuberculosis
4.2.1.1 zonisamide
-
 Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
4.2.1.1 Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
4.2.1.1 glutathione Sepharose 4B column chromatography and sulfonamide affinity chromatography Mycobacterium tuberculosis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.2.1.1 CO2 + H2O
-
 Mycobacterium tuberculosis H2CO3
-
 r

Synonyms

EC Number Synonyms Comment Organism
4.2.1.1 beta-carbonic anhydrase
-
 Mycobacterium tuberculosis
4.2.1.1 CA 1
-
 Mycobacterium tuberculosis
4.2.1.1 Rv1284
-
 Mycobacterium tuberculosis

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
4.2.1.1 390000
-
 CO2 at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.2.1.1 0.000097
-
 indisulam at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000186
-
 4-amino-3-bromobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000481
-
 acetazolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000612
-
 topiramate at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000612
-
 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000744
-
 dorzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00075
-
 4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000781
-
 methazolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00081
-
 benzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000839
-
 brinzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000853
-
 4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000872
-
 4,5-dichloro-benzene-1,3-disulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.000905
-
 5-[[(4-aminophenyl)sulfonyl]amino]-1,3,4-thiadiazole-2-sulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00103
-
 ethoxzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00172
-
 4-amino-6-chlorobenzene-1,3-disulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.0023
-
 sulpiride at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00492
-
 4-methylbenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00516
-
 sulthiame at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00551
-
 4-(2-hydroxyethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00748
-
 5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00752
-
 4-amino-3-chlorobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00771
-
 4-amino-3-iodobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00793
-
 3-(4-sulfamoylphenyl)propanoic acid at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00796
-
 saccharin at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.0081
-
 4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00821
-
 4-sulfamoylbenzoic acid at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00869
-
 4-(aminomethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00874
-
 4-amino-3-fluorobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00923
-
 2-aminobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00956
-
 4-(2-aminoethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00956
-
 4-(hydroxymethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.00984
-
 4-Aminobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.01035
-
 celecoxib at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.01154
-
 5-amino-1,3,4-thiadiazole-2-sulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.01265
-
 5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.01297
-
 valdecoxib at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
4.2.1.1 0.02868
-
 zonisamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis

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 37000
-
 CO2 at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis