Literature summary for 7.6.2.2 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.

Search for more literature for 7.6.2.2

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

KM Value [mM]

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

Organism

Organism	UniProt	Comment	Textmining
Streptomyces peucetius	P32010	-	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
DrrAB	-	Streptomyces peucetius

Ki Value [mM]

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

IC50 Value

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

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)