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Literature summary for 7.6.2.2 extracted from

  • Zolnerciks, J.K.; Akkaya, B.G.; Snippe, M.; Chiba, P.; Seelig, A.; Linton, K.J.
    The Q loops of the human multidrug resistance transporter ABCB1 are necessary to couple drug binding to the ATP catalytic cycle (2014), FASEB J., 28, 4335-4346.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expressed in High Five insect cells and HEK-293T cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
Q1118A the mutant with 8.1% of wild type activity accumulates low levels of Bodipy-verapamil Homo sapiens
Q475A the mutant with 9.5% of wild type activity accumulates low levels of Bodipy-verapamil Homo sapiens
Q475A/Q1118A the mutant accumulates more levels of Bodipy-verapamil compared to the wild type enzyme Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.284
-
 ATP mutant enzyme Q475A, in the absence of nicardipine, at 37°C, pH not specified in the publication Homo sapiens
0.327
-
 ATP wild type enzyme, in the absence of nicardipine, at 37°C, pH not specified in the publication Homo sapiens
0.573
-
 ATP mutant enzyme Q1118A, in the absence of nicardipine, at 37°C, pH not specified in the publication Homo sapiens
0.746
-
 ATP wild type enzyme, in the presence of 0.05 mM nicardipine, at 37°C, pH not specified in the publication Homo sapiens
2.34
-
 ATP mutant enzyme Q1118A, in the presence of 0.05 mM nicardipine, at 37°C, pH not specified in the publication Homo sapiens
2.37
-
 ATP mutant enzyme Q475A, in the presence of 0.05 mM nicardipine, at 37°C, pH not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA resin column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + Bodipy-verapamil/in
-
 Homo sapiens ADP + phosphate + Bodipy-verapamil/out
-
 ?
ATP + H2O + nicardipine/in
-
 Homo sapiens ADP + phosphate + nicardipine/out
-
 ?

Synonyms

Synonyms Comment Organism
ABCB1
-
 Homo sapiens
MDR1
-
 Homo sapiens
P-glycoprotein
-
 Homo sapiens