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Literature summary for 7.6.2.2 extracted from

  • Puri, N.; Gaur, M.; Sharma, M.; Shukla, S.; Ambudkar, S.V.; Prasad, R.
    The amino acid residues of transmembrane helix 5 of multidrug resistance protein CaCdr1p of Candida albicans are involved in substrate specificity and drug transport (2009), Biochim. Biophys. Acta, 1788, 1752-1761.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of Cdr1p as a GFP-tagged protein in plasma membrane of Saccharomyces cerevisiae Candida albicans

Protein Variants

Protein Variants Comment Organism
A666G the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs, the mutant displays a hyperresistant phenotype towards fluconazole comparable to wild type Candida albicans
F673A the mutant shows a reduction in both Km and Vmax values of ATPase activity when compared to wild-type Cdr1p-GFP, and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
G672A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
I675A the mutant shows a reduction in both Km and Vmax values of ATPase activity when compared to wild-type Cdr1p-GFP, and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
L663A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
L664A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
M667A the mutant shows a reduction in both Km and Vmax values of ATPase activity when compared to wild-type Cdr1p-GFP, and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
additional information substrate specificities of transmembrane segment mutants, overview Candida albicans
P659A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
P676A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
P678A the mutant shows a reduction in both Km and Vmax values of ATPase activity when compared to wild-type Cdr1p-GFP, and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
T671A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
T677A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
V668A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans
V674A the mutant shows an uncoupling of ATPase and drug transport and displays a selective loss of resistance to one or more of the tested drugs Candida albicans

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.58
-
ATP pH 7.5, 30°C, recombinant mutant I675A Candida albicans
2.68
-
ATP pH 7.5, 30°C, recombinant mutant M667A Candida albicans
2.7
-
ATP pH 7.5, 30°C, recombinant mutant P678A Candida albicans
3.62
-
ATP pH 7.5, 30°C, recombinant mutant L663A Candida albicans
3.62
-
ATP pH 7.5, 30°C, recombinant mutant Y670A Candida albicans
3.73
-
ATP pH 7.5, 30°C, recombinant mutant L665A Candida albicans
3.92
-
ATP pH 7.5, 30°C, recombinant mutant P673A Candida albicans
4.04
-
ATP pH 7.5, 30°C, recombinant mutant I669A Candida albicans
4.06
-
ATP pH 7.5, 30°C, recombinant mutant L664A Candida albicans
4.36
-
ATP pH 7.5, 30°C, recombinant mutant T671A Candida albicans
4.75
-
ATP pH 7.5, 30°C, recombinant mutant V674A Candida albicans
4.82
-
ATP pH 7.5, 30°C, recombinant mutant P659A Candida albicans
4.83
-
ATP pH 7.5, 30°C, recombinant mutant P676A Candida albicans
4.9
-
ATP pH 7.5, 30°C, recombinant mutant T677A Candida albicans
5.21
-
ATP pH 7.5, 30°C, recombinant mutant G672A Candida albicans
5.69
-
ATP pH 7.5, 30°C, recombinant mutant V668A Candida albicans
5.71
-
ATP pH 7.5, 30°C, recombinant mutant V662A Candida albicans
6.08
-
ATP pH 7.5, 30°C, recombinant mutant A666G Candida albicans
6.39
-
ATP pH 7.5, 30°C, recombinant wild-type enzyme Candida albicans
7.19
-
ATP pH 7.5, 30°C, recombinant mutant A660G Candida albicans
7.55
-
ATP pH 7.5, 30°C, recombinant mutant T658A Candida albicans

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane transmembrane protein Candida albicans 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Candida albicans

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic/in Candida albicans importance of Candida drug resistance protein Cdr1p of pathogenic Candida albicans in azole resistance ADP + phosphate + xenobiotic/out
-
?

Organism

Organism UniProt Comment Textmining
Candida albicans
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
substrate specificities of transmembrane segment mutants, overview Candida albicans

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + anisomycin/in
-
Candida albicans ADP + phosphate + anisomycin/out
-
?
ATP + H2O + beta-estradiol/in
-
Candida albicans ADP + phosphate + beta-estradiol/out
-
?
ATP + H2O + cycloheximide /in
-
Candida albicans ADP + phosphate + cycloheximide /out
-
?
ATP + H2O + fluconazole/in
-
Candida albicans ADP + phosphate + fluconazole/out
-
?
ATP + H2O + itraconazole/in
-
Candida albicans ADP + phosphate + itraconazole/out
-
?
ATP + H2O + ketoconazole/in
-
Candida albicans ADP + phosphate + ketoconazole/out
-
?
ATP + H2O + miconazole/in
-
Candida albicans ADP + phosphate + miconazole/out
-
?
ATP + H2O + oligomycin/in
-
Candida albicans ADP + phosphate + oligomycin/out
-
?
ATP + H2O + progesterone/in
-
Candida albicans ADP + phosphate + progesterone/out
-
?
ATP + H2O + rhodamine 6G/in
-
Candida albicans ADP + phosphate + rhodamine 6G/out
-
?
ATP + H2O + xenobiotic/in
-
Candida albicans ADP + phosphate + xenobiotic/out
-
?
ATP + H2O + xenobiotic/in importance of Candida drug resistance protein Cdr1p of pathogenic Candida albicans in azole resistance Candida albicans ADP + phosphate + xenobiotic/out
-
?

Synonyms

Synonyms Comment Organism
Cdr1p
-
Candida albicans
multidrug resistance protein
-
Candida albicans

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Candida albicans

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Candida albicans

Cofactor

Cofactor Comment Organism Structure
ATP
-
Candida albicans