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Literature summary for 4.2.1.1 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
Search for more literature for 4.2.1.1

Cloned(Commentary)

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000097
-
 indisulam at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.000481
-
 acetazolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.000612
-
 topiramate at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.000744
-
 dorzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.000781
-
 methazolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.00081
-
 benzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.000839
-
 brinzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
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
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
0.00103
-
 ethoxzolamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.0023
-
 sulpiride at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.00492
-
 4-methylbenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.00516
-
 sulthiame at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
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
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
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
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
0.00796
-
 saccharin at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.00821
-
 4-sulfamoylbenzoic acid at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.00869
-
 4-(aminomethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.00923
-
 2-aminobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
0.00956
-
 4-(hydroxymethyl)benzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.00984
-
 4-Aminobenzenesulfonamide at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
0.01035
-
 celecoxib at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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
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
0.01297
-
 valdecoxib at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis
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]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
37000
-
 CO2 at 20°C and pH 8.3, in 20 mM Tris-HCl buffer and 20 mM NaCl Mycobacterium tuberculosis