Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 7.2.2.19 extracted from

  • Abe, K.; Shimokawa, J.; Naito, M.; Munson, K.; Vagin, O.; Sachs, G.; Suzuki, H.; Tani, K.; Fujiyoshi, Y.
    The cryo-EM structure of gastric H+,K+-ATPase with bound BYK99, a high-affinity member of K+-competitive, imidazo[1,2-a]pyridine inhibitors (2017), Sci. Rep., 7, 6632 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.2.2.19

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293S GnT1 cells Sus scrofa

Protein Variants

Protein Variants Comment Organism
D136A the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
D136F the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
D136I the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
D136L the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
D137A the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, BYK99 and BYK73) Sus scrofa
D137F the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-CN-, BYK99 and BYK73) Sus scrofa
D137I the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, and BYK99) Sus scrofa
D137L the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
D138I the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
L139A the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
L139F the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
L139I the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
L141A the mutant has low ATPase activity Sus scrofa
L141F the mutant has low ATPase activity Sus scrofa
L141I the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
N138A the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
N138F the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
N138L the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (BYK99 and BYK73) Sus scrofa
Y140A the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
Y140F the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
Y140I the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa
Y140L the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) Sus scrofa

Inhibitors

Inhibitors Comment Organism Structure
(7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol
-
 Sus scrofa
(7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol high-affinity K+-competitive inhibitor Sus scrofa
8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine
-
 Sus scrofa
BYK73 i.e. (7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol Sus scrofa
BYK99 i.e. (7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol, high-affinity K+-competitive inhibitor Sus scrofa
SCH-CN- i.e. 8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine Sus scrofa
SCH-Me- i.e. [8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile Sus scrofa
SCH28080 i.e. 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile Sus scrofa
[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile
-
 Sus scrofa
[8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile
-
 Sus scrofa

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + H+[side 1] + K+[side 2] Sus scrofa
-
 ADP + phosphate + H+[side 2] + K+[side 1]
-
 ?

Organism

Organism UniProt Comment Textmining
Sus scrofa P19156 and P18434 subunits alpha and beta
-

Source Tissue

Source Tissue Comment Organism Textmining
stomach
-
 Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + H+[side 1] + K+[side 2]
-
 Sus scrofa ADP + phosphate + H+[side 2] + K+[side 1]
-
 ?

Synonyms

Synonyms Comment Organism
H+,K+-ATPase
-
 Sus scrofa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000058
-
 8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0000058
-
 BYK99 wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.00015
-
 SCH28080 wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0015
-
 (7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0032
-
 [8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0032
-
 SCH-CN- wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0049
-
 (7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.0049
-
 BYK73 wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.011
-
 [8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile wild type enzyme, at pH 7.6 and 37°C Sus scrofa
0.011
-
 SCH-Me- wild type enzyme, at pH 7.6 and 37°C Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000077
-
 wild type enzyme, at pH 7.6 and 37°C Sus scrofa (7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol
0.0011
-
 at pH 7.6 and 37°C Sus scrofa SCH28080
0.011
-
 wild type enzyme, at pH 7.6 and 37°C Sus scrofa [8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile
0.029
-
 wild type enzyme, at pH 7.6 and 37°C Sus scrofa (7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol
0.054
-
 wild type enzyme, at pH 7.6 and 37°C Sus scrofa [8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile
0.11
-
 wild type enzyme, at pH 7.6 and 37°C Sus scrofa 8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine