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Literature summary for 7.2.2.19 extracted from

  • Vagin, O.; Munson, K.; Lambrecht, N.; Karlish, S.J.; Sachs, G.
    Mutational analysis of the K+-competitive inhibitor site of gastric H,K-ATPase (2001), Biochemistry, 40, 7480-7490.
    View publication on PubMed
Search for more literature for 7.2.2.19

Activating Compound

Activating Compound Comment Organism Structure
NH4+ 20 mM, increases activity by about 4.5fold Oryctolagus cuniculus

Protein Variants

Protein Variants Comment Organism
D824A complete loss of NH4+-stimulated H,K-ATPase activity, the Ki value for SCH28080 is decreased to about 78% of the wild-type value, NH4+-independent H,K-ATPase activity is 3.2fold higher than the wild-type value Oryctolagus cuniculus
D824A NH4+-independent H,K-ATPase activity is 97% of the wild-type value Oryctolagus cuniculus
D824E NH4+-independent H,K-ATPase activity is 2.8fold higher than the wild-type value Oryctolagus cuniculus
D824N NH4+-independent H,K-ATPase activity is 46% of the wild-type value Oryctolagus cuniculus
E343A complete loss of NH4+-stimulated H,K-ATPase activity, NH4+-independent H,K-ATPase activity is 80% of the wild-type value Oryctolagus cuniculus
E343D complete loss of NH4+-stimulated H,K-ATPase activity, NH4+-independent H,K-ATPase activity is 39% of the wild-type value Oryctolagus cuniculus
E343Q the apparent Km-value for NH4+ is increased about 4fold, the Ki value for SCH28080 is increased about 2fold, NH4+-independent H,K-ATPase activity is 83% of the wild-type value Oryctolagus cuniculus
E795D the apparent Km-value for NH4+ is increased about 3fold, the Ki value for SCH28080 is increased about 11fold, NH4+-independent H,K-ATPase activity is 29% of the wild-type value Oryctolagus cuniculus
E795Q the Ki value for SCH28080 is increased 1.3fold, NH4+-independent H,K-ATPase activity is 2.3fold higher than the wild-type value Oryctolagus cuniculus
E820A complete loss of NH4+-stimulated H,K-ATPase activity Oryctolagus cuniculus
E820D the Ki value for SCH28080 is increased 2.7fold, NH4+-independent H,K-ATPase activity is 1.5fold higher than the wild-type value Oryctolagus cuniculus
E936D the apparent Km-value for NH4+ is increased about 2fold. the Ki value for SCH28080 is increased 2.5fold, NH4+-independent H,K-ATPase activity is 1.7fold higher than the wild-type value Oryctolagus cuniculus
E936Q NH4+-independent H,K-ATPase activity is 2.95fold higher than the wild-type value Oryctolagus cuniculus
E936V complete loss of NH4+-stimulated H,K-ATPase activity Oryctolagus cuniculus
K791A complete loss of NH4+-stimulated H,K-ATPase activity, NH4+-independent H,K-ATPase activity is 17% of the wild-type value Oryctolagus cuniculus
K791S the apparent Km-value for NH4+ is increased about 2fold. the Ki value for SCH28080 is increased 20.7fold, NH4+-independent H,K-ATPase activity is 51% of the wild-type value Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
SCH28080
-
 Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus P18597 beta-subunit
-
Oryctolagus cuniculus P27112 alpha-subunit
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + H+/in + K+/out
-
 Oryctolagus cuniculus ADP + phosphate + H+/out + K+/in
-
 ?

Synonyms

Synonyms Comment Organism
gastric H,K-ATPase
-
 Oryctolagus cuniculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00005
-
 SCH28080 pH 7.4, 37°C, mutant enzyme D824A Oryctolagus cuniculus
0.000064
-
 SCH28080 pH 7.4, 37°C, wild-type enzyme Oryctolagus cuniculus
0.000086
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E795Q Oryctolagus cuniculus
0.000122
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E343Q Oryctolagus cuniculus
0.000153
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E936D Oryctolagus cuniculus
0.000162
-
 SCH28080 pH 7.4, 37°C, mutant enzyme D824E Oryctolagus cuniculus
0.000174
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E820D Oryctolagus cuniculus
0.0007
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E795D Oryctolagus cuniculus
0.00084
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E936Q Oryctolagus cuniculus
0.001325
-
 SCH28080 pH 7.4, 37°C, mutant enzyme K791S Oryctolagus cuniculus