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Literature summary extracted from

  • Crowley, E.; OMara, M.L.; Reynolds, C.; Tieleman, D.P.; Storm, J.; Kerr, I.D.; Callaghan, R.
    Transmembrane helix 12 modulates progression of the ATP catalytic cycle in ABCB1 (2009), Biochemistry, 48, 6249-6254.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
7.6.2.2 nicardipine
-
 Homo sapiens
7.6.2.2 vinblastine
-
 Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 expression of His-tagged ABCB1 in Trichoplusia ni high-five cells using the baculovirus expression system Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
7.6.2.2 A980C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 F978C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 F994C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 G984C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 G989C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 L976C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 M986C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 additional information construction of a series of single cysteine isoforms of ABCB1, selection of mutations based on a direct comparison of the sequences of TM6 and TM12 and by inspection of our Sav1866-directed homology model of human ABCB1. 11 single cysteine isoforms generated provide both a longitudinal and rotational coverage of the alpha helix. Introduction of cysteine residues can affect the ATP binding, overview Homo sapiens
7.6.2.2 Q990C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 S992C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 V982C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens
7.6.2.2 V988C site-directed mutagenesis, the mutant shows altered substrate transport activity and activation by the substrates, e.g. vinblastine and nicardipine, compared to the wild-type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 azido-ATP competitive, binding activity of wild-type and mutant enzymes, overview Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
7.6.2.2 membrane
-
 Homo sapiens 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
7.6.2.2 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 ATP + H2O + xenobiotic/in Homo sapiens
-
 ADP + phosphate + xenobiotic/out
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
7.6.2.2 recombinant His-tagged ABCB1 from Trichoplusia ni high-five cells by metal affinity chromatography Homo sapiens

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
7.6.2.2 additional information
-
 activities of purified wild-type and mutant enzymes, overview Homo sapiens
7.6.2.2 0.02
-
 about, purified recombinant mutant F978C Homo sapiens
7.6.2.2 0.25
-
 purified recombinant wild-type enzyme Homo sapiens
7.6.2.2 0.5
-
 purified recombinant mutant A980C Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + nicardipine/in
-
 Homo sapiens ADP + phosphate + nicardipine/out
-
 ?
7.6.2.2 ATP + H2O + vinblastine/in
-
 Homo sapiens ADP + phosphate + vinblastine/out
-
 ?
7.6.2.2 ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
 Homo sapiens
7.6.2.2 More ABCB1, or P-glycoprotein, is a member of the ATP binding cassette protein family Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.6.2.2 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6.2.2 7.4
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
7.6.2.2 ATP
-
 Homo sapiens