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Literature summary for 7.2.2.19 extracted from

  • Vagin, O.; Denevich, S.; Munson, K.; Sachs, G.
    SCH28080, a K+-competitive inhibitor of the gastric H,K-ATPase, binds near the M5-6 luminal loop, preventing K+ access to the ion binding domain (2002), Biochemistry, 41, 12755-12762.
    View publication on PubMed
Search for more literature for 7.2.2.19

Protein Variants

Protein Variants Comment Organism
C813A mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
C813S mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
C813T mutant enzyme shows 9fold loss of SCH28080 affinity Oryctolagus cuniculus
E914Q mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
F818C mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
F917Y mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
F932L mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
G918E mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
I803L mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
I814F mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
I814V mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
I816L mutation reduces affinity towards the inhibitor SCH28080 by about 10fold, resulting in noncompetitive kinetics Oryctolagus cuniculus
I819L mutant enzyme shows mixed inhibition with SCH28080, no change in inhibitor affinity Oryctolagus cuniculus
I940A mutation reduces affinity to the inhibitor SCH28080 by about 10fold and results in mixed inhibition Oryctolagus cuniculus
L809F mutation results in a about 100fold decrease in affinity towards SCH28080 Oryctolagus cuniculus
L809V mutation reduces affinity towards the inhibitor SCH28080 by about 10fold, resulting in noncompetitive kinetics Oryctolagus cuniculus
L811F mutation reduces affinity to the inhibitor SCH28080 by about 10fold and results in mixed inhibition Oryctolagus cuniculus
L811V mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
M937V mutation reduces affinity towards the inhibitor SCH28080 by about 10fold, resulting in noncompetitive kinetics Oryctolagus cuniculus
P798C mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
P810A mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
P810G mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
Q905N mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
Q923V mutant enzyme shows mixed inhibition with SCH28080, no change in inhibitor affinity Oryctolagus cuniculus
S806N mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
T823V mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
T929L mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
V807I mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
Y799F mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
Y802F mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus
Y802L mutation reduces the affinity for SCH28080 up to 10fold without affecting the nature of the kinetics Oryctolagus cuniculus
Y922I mutation reduces affinity to the inhibitor SCH28080 by about 10fold and results in mixed inhibition Oryctolagus cuniculus
Y925A mutant enzyme shows mixed inhibition with SCH28080, no change in inhibitor affinity Oryctolagus cuniculus
Y925F mutation reduces affinity towards the inhibitor SCH28080 by about 10fold, resulting in noncompetitive kinetics Oryctolagus cuniculus
Y928H mutation has no effect on inhibitor kinetics of SCH28080 Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
SCH28080 strictly competitive with respect to K+ or NH4+, binds near the M5-6 luminal loop, preventing K+ access to the ion binding domain Oryctolagus cuniculus

Organism

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

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000028
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I819L Oryctolagus cuniculus
0.000063
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Q905N Oryctolagus cuniculus
0.000064
-
 SCH28080 pH 7.4, 37°C, wild-type enzyme Oryctolagus cuniculus
0.000065
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Q923V Oryctolagus cuniculus
0.000065
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y802F Oryctolagus cuniculus
0.000066
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Q924E Oryctolagus cuniculus
0.000079
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I803L Oryctolagus cuniculus
0.000082
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y925A Oryctolagus cuniculus
0.000083
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y928H Oryctolagus cuniculus
0.00009
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y799F Oryctolagus cuniculus
0.000095
-
 SCH28080 pH 7.4, 37°C, mutant enzyme L811V Oryctolagus cuniculus
0.000096
-
 SCH28080 pH 7.4, 37°C, mutant enzyme V807I Oryctolagus cuniculus
0.000102
-
 SCH28080 pH 7.4, 37°C, mutant enzyme S806N Oryctolagus cuniculus
0.000125
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y802L Oryctolagus cuniculus
0.000133
-
 SCH28080 pH 7.4, 37°C, mutant enzyme T823V Oryctolagus cuniculus
0.000141
-
 SCH28080 pH 7.4, 37°C, mutant enzyme E914Q Oryctolagus cuniculus
0.000151
-
 SCH28080 pH 7.4, 37°C, mutant enzyme G918E and mutant enzyme Y922I Oryctolagus cuniculus
0.000163
-
 SCH28080 pH 7.4, 37°C, mutant enzyme P798C Oryctolagus cuniculus
0.000169
-
 SCH28080 pH 7.4, 37°C, mutant enzyme C813S Oryctolagus cuniculus
0.000182
-
 SCH28080 pH 7.4, 37°C, mutant enzyme C813A Oryctolagus cuniculus
0.000182
-
 SCH28080 pH 7.4, 37°C, mutant enzyme F917Y Oryctolagus cuniculus
0.0002
-
 SCH28080 pH 7.4, 37°C, mutant enzyme F932L Oryctolagus cuniculus
0.000248
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I940A Oryctolagus cuniculus
0.000249
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I814F Oryctolagus cuniculus
0.000265
-
 SCH28080 pH 7.4, 37°C, mutant enzyme F818C Oryctolagus cuniculus
0.000281
-
 SCH28080 pH 7.4, 37°C, mutant enzyme M937V Oryctolagus cuniculus
0.000281
-
 SCH28080 pH 7.4, 37°C, mutant enzyme P810A Oryctolagus cuniculus
0.000288
-
 SCH28080 pH 7.4, 37°C, mutant enzyme L809V Oryctolagus cuniculus
0.000298
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I814V Oryctolagus cuniculus
0.000309
-
 SCH28080 pH 7.4, 37°C, mutant enzyme I816L Oryctolagus cuniculus
0.000372
-
 SCH28080 pH 7.4, 37°C, mutant enzyme Y925F Oryctolagus cuniculus
0.000512
-
 SCH28080 pH 7.4, 37°C, mutant enzyme T929L Oryctolagus cuniculus
0.000563
-
 SCH28080 pH 7.4, 37°C, mutant enzyme P810G Oryctolagus cuniculus
0.000586
-
 SCH28080 pH 7.4, 37°C, mutant enzyme C813T Oryctolagus cuniculus
0.000625
-
 SCH28080 pH 7.4, 37°C, mutant enzyme L811F Oryctolagus cuniculus
0.00615
-
 SCH28080 pH 7.4, 37°C, mutant enzyme L809F Oryctolagus cuniculus