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Literature summary for 7.6.2.2 extracted from
- Transmembrane helix 12 modulates progression of the ATP catalytic cycle in ABCB1 (2009), Biochemistry, 48, 6249-6254.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| nicardipine | - |
Homo sapiens |  |
| vinblastine | - |
Homo sapiens | |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of His-tagged ABCB1 in Trichoplusia ni high-five cells using the baculovirus expression system | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| azido-ATP | competitive, binding activity of wild-type and mutant enzymes, overview | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | - |
Homo sapiens | 16020 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + xenobiotic/in | Homo sapiens | - |
ADP + phosphate + xenobiotic/out | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged ABCB1 from Trichoplusia ni high-five cells by metal affinity chromatography | Homo sapiens |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
activities of purified wild-type and mutant enzymes, overview | Homo sapiens |
| 0.02 | - |
about, purified recombinant mutant F978C | Homo sapiens |
| 0.25 | - |
purified recombinant wild-type enzyme | Homo sapiens |
| 0.5 | - |
purified recombinant mutant A980C | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + nicardipine/in | - |
Homo sapiens | ADP + phosphate + nicardipine/out | - |
? | |
| ATP + H2O + vinblastine/in | - |
Homo sapiens | ADP + phosphate + vinblastine/out | - |
? | |
| ATP + H2O + xenobiotic/in | - |
Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ABCB1 | - |
Homo sapiens |
| More | ABCB1, or P-glycoprotein, is a member of the ATP binding cassette protein family | Homo sapiens |
| P-glycoprotein | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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Release 2023.1 (January 2023)
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