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Literature summary for 4.2.1.1 extracted from

  • Baranauskiene, L.; Hilvo, M.; Matuliene, J.; Golovenko, D.; Manakova, E.; Dudutiene, V.; Michailoviene, V.; Torresan, J.; Jachno, J.; Parkkila, S.; Maresca, A.; Supuran, C.T.; Grazulis, S.; Matulis, D.
    Inhibition and binding studies of carbonic anhydrase isozymes I, II and IX with benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides (2010), J. Enzyme Inhib. Med. Chem., 25, 863-870.
    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 using the baculovirus-insect cell expression system Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
isoform CA II, sitting drop vapor diffusion method, using 0.1 M sodium bicine, 0.2 M ammonium sulfate and 2 M sodium malonate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,1,1-trifluoromethanesulfonamide
-
 Homo sapiens
1,1-dimethyl-4-(7-sulfamoyl-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazol-3-yl)piperazin-1-ium iodide
-
 Homo sapiens
3-(4-methylpiperazin-1-yl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
3-(methylsulfanyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
3-(methylsulfonyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
3-(phenylsulfanyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
3-chloro-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
3-morpholin-4-yl-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide
-
 Homo sapiens
acetazolamide
-
 Homo sapiens
methazolamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16790 isozyme CA IX
-

Purification (Commentary)

Purification (Comment) Organism
Sepharose-IDA-Ni+2 column chromatography, S-Sepharose column chromatography, gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CO2 + H2O
-
 Homo sapiens H2CO3
-
 r

Synonyms

Synonyms Comment Organism
CA I isozyme Homo sapiens
CA II isozyme Homo sapiens
CA IX isozyme Homo sapiens
carbonic anhydrase
-
 Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
55 60 the melting temperature is around 55°C without the addition of ligand, and shifts to 60°C or higher when the added ligand binds and stabilizes the protein Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000009
-
 3-morpholin-4-yl-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA II, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.000033
-
 3-chloro-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA II, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.000057
-
 3-(methylsulfanyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA II, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00015
-
 3-(methylsulfanyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA I, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00021
-
 3-morpholin-4-yl-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA I, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00021
-
 3-morpholin-4-yl-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA IX, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00046
-
 4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA II, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00051
-
 3-(methylsulfanyl)-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA IX, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00066
-
 3-chloro-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA I, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.00072
-
 4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA IX, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.001
-
 3-chloro-4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA IX, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens
0.0021
-
 4H-[1,2,3]thiadiazolo[3,4-a]benzimidazole-7-sulfonamide isoform CA I, in 10 mM HEPES (pH 7.5), 0.1 M Na2SO4 Homo sapiens