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Literature summary for 7.6.2.2 extracted from

  • Siarheyeva, A.; Liu, R.; Sharom, F.J.
    Characterization of an asymmetric occluded state of P-glycoprotein with two bound nucleotides: implications for catalysis (2010), J. Biol. Chem., 285, 7575-7586.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Inhibitors

Inhibitors Comment Organism Structure
ADP
-
 Cricetulus griseus
AMP-imidodiphosphate
-
 Cricetulus griseus
ATPgammaS existence of two binding sites for ATPS with remarkably different binding affinities. One site binds ATPgammaS with Kd of 6 microM and the second binds ATPgammaS with Kd of 0.74 mM Cricetulus griseus
beta,gamma-methylene adenosine 5'-triphosphate
-
 Cricetulus griseus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.11
-
 8-azido-ATP pH 7.5, 37°C Cricetulus griseus
0.53
-
 ATP pH 7.5, 37°C Cricetulus griseus
1.3
-
 epsilon-ATP pH 7.5, 37°C Cricetulus griseus

Organism

Organism UniProt Comment Textmining
Cricetulus griseus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
CHRB-30 cell multidrug-resistant Chinese hamster ovary cells Cricetulus griseus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
8-azido-ATP + H2O
-
 Cricetulus griseus ? + phosphate
-
 ?
ATP + H2O
-
 Cricetulus griseus ADP + phosphate
-
 ?
epsilon-ATP + H2O
-
 Cricetulus griseus ? + phosphate
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.36
-
 ATPgammaS pH 7.5, 37°C Cricetulus griseus
0.53
-
 ADP pH 7.5, 37°C Cricetulus griseus
1.6
-
 AMP-imidodiphosphate pH 7.5, 37°C, sigmoidal inhibition plot, Hill coefficient n=1.77 Cricetulus griseus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.006
-
 pH 7.5, 37°C Cricetulus griseus beta,gamma-methylene adenosine 5'-triphosphate