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Literature summary for 7.6.2.2 extracted from

  • Swartz, D.J.; Mok, L.; Botta, S.K.; Singh, A.; Altenberg, G.A.; Urbatsch, I.L.
    Directed evolution of P-glycoprotein cysteines reveals site-specific, non-conservative substitutions that preserve multidrug resistance (2014), Biosci. Rep., 34, e00116.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Saccharomyces cerevisiae JPY201 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclosporine A
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
120000
-
x * 120000, SDS-PAGE 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
Ni-NTA resin column chromatography and Superose 6B column chromatography Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.5
-
with verapamil and ATP as substrates, at pH 7.4 and 37°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + daunorubicin/in
-
Homo sapiens ADP + phosphate + daunorubicin/out
-
?
ATP + H2O + doxorubicin/in
-
Homo sapiens ADP + phosphate + doxorubicin/out
-
?
ATP + H2O + verapamil/in
-
Homo sapiens ADP + phosphate + verapamil/out
-
?
ATP + H2O + xenobiotic/in
-
Homo sapiens ADP + phosphate + xenobiotic/out
-
?

Subunits

Subunits Comment Organism
? x * 120000, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
ABCB1
-
Homo sapiens
MDR1
-
Homo sapiens
P-glycoprotein
-
Homo sapiens
Pgp
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
cyclosporine A pH and temperature not specified in the publication Homo sapiens