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Literature summary extracted from

  • Li, W.; Sharma, M.; Kaur, P.
    The DrrAB efflux system of Streptomyces peucetius is a multidrug transporter of broad substrate specificity (2014), J. Biol. Chem., 289, 12633-12646.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 expressed in Escherichia coli LE39 cells Streptomyces peucetius

Protein Variants

EC Number Protein Variants Comment Organism
7.6.2.2 E165Q the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 G44A the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 G44S the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 K47R the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 Q197H the mutant shows strongly reduced activity (less than 20%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 Q197H/Y198H the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 Q197H/Y198R the mutant shows about 35% activity compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 S141R the mutant shows strongly reduced activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius
7.6.2.2 Y198R the mutant shows about 30% activity (less than 10%) compared to the wild type enzyme Streptomyces peucetius

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 Colchicine
-
 Streptomyces peucetius
7.6.2.2 Ethidium bromide
-
 Streptomyces peucetius
7.6.2.2 Hoechst 33342 inhibition of doxorubicin transport by Hoechst 33342 occurs by a competitive mechanism Streptomyces peucetius
7.6.2.2 additional information not inhibited by rhodamine 123, rhodamine 6G, rhodamine B, quinine, and tetramethylrhodamine Streptomyces peucetius
7.6.2.2 quinidine
-
 Streptomyces peucetius
7.6.2.2 rifampicin inhibition of doxorubicin transport by rifampicin occurs by a competitive mechanism Streptomyces peucetius
7.6.2.2 vanadate complete inhibition of doxorubicin transport at 0.1 mM vanadate Streptomyces peucetius
7.6.2.2 verapamil inhibits transport of doxorubicin by a non-competitive mechanism Streptomyces peucetius
7.6.2.2 vinblastine
-
 Streptomyces peucetius

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
7.6.2.2 0.00039
-
 doxorubicin/in in the presence of ATP, at pH 7.5 and 37°C Streptomyces peucetius
7.6.2.2 0.00078
-
 Hoechst 33342/in in the presence of ATP, at pH 7.5 and 37°C Streptomyces peucetius
7.6.2.2 0.021
-
 ethidium bromide/in in the presence of ATP, at pH 7.5 and 37°C Streptomyces peucetius

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Streptomyces peucetius P32010
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + doxorubicin/in
-
 Streptomyces peucetius ADP + phosphate + doxorubicin/out
-
 ?
7.6.2.2 ATP + H2O + ethidium bromide/in
-
 Streptomyces peucetius ADP + phosphate + ethidium bromide/out
-
 ?
7.6.2.2 ATP + H2O + Hoechst 33342/in
-
 Streptomyces peucetius ADP + phosphate + Hoechst 33342/out
-
 ?
7.6.2.2 ATP + H2O + rifampicin/in
-
 Streptomyces peucetius ADP + phosphate + rifampicin/out
-
 ?
7.6.2.2 ATP + H2O + verapamil/in
-
 Streptomyces peucetius ADP + phosphate + verapamil/out
-
 ?
7.6.2.2 ATP + H2O + vinblastine/in
-
 Streptomyces peucetius ADP + phosphate + vinblastine/out
-
 ?
7.6.2.2 GTP + H2O + doxorubicin/in highest efficiency Streptomyces peucetius GDP + phosphate + doxorubicin/out
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 DrrAB
-
 Streptomyces peucetius

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
7.6.2.2 0.0006
-
 Hoechst 33342 at pH 7.5 and 37°C Streptomyces peucetius
7.6.2.2 0.0094
-
 verapamil at pH 7.5 and 37°C Streptomyces peucetius
7.6.2.2 0.012
-
 rifampicin at pH 7.5 and 37°C Streptomyces peucetius

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.6.2.2 0.00051
-
 at pH 7.5 and 37°C Streptomyces peucetius Hoechst 33342
7.6.2.2 0.0078
-
 at pH 7.5 and 37°C Streptomyces peucetius vinblastine
7.6.2.2 0.009
-
 at pH 7.5 and 37°C Streptomyces peucetius verapamil
7.6.2.2 0.011
-
 at pH 7.5 and 37°C Streptomyces peucetius vanadate
7.6.2.2 0.014
-
 at pH 7.5 and 37°C Streptomyces peucetius rifampicin
7.6.2.2 0.033
-
 at pH 7.5 and 37°C Streptomyces peucetius Ethidium bromide
7.6.2.2 0.049
-
 at pH 7.5 and 37°C Streptomyces peucetius quinidine
7.6.2.2 0.062
-
 at pH 7.5 and 37°C Streptomyces peucetius Colchicine