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Literature summary for 7.6.2.2 extracted from

  • Yang, Z.; Wu, D.; Bui, T.; Ho, R.J.
    A novel human multidrug resistance gene MDR1 variant G571A (G191R) modulates cancer drug resistance and efflux transport (2008), J. Pharmacol. Exp. Ther., 327, 474-481.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
gene MDR1, expression of wild-type and mutant MDR1571A enzymes in HEK-293 cells. MDR1 571 genotypes in leukemia patients, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
G571A/G191R a naturally occuring mutant, the genetic variation modulates cancer drug resistance and efflux transport, minimal effect on doxorubicin and daunorubicin, the MDR1-dependent resistance on vinblastine, vincristine, paclitaxel, and etoposide is reduced by approximately 5fold, 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 P08183 human multidrug resistance gene MDR1 encoding a membrane-bound transporter P-glycoprotein
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
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 + etoposide/in
-
Homo sapiens ADP + phosphate + etoposide/out
-
?
ATP + H2O + paclitaxel/in
-
Homo sapiens ADP + phosphate + paclitaxel/out
-
?
ATP + H2O + rhodamine 123/in
-
Homo sapiens ADP + phosphate + rhodamine 123/out
-
?
ATP + H2O + vinblastine sulfate/in
-
Homo sapiens ADP + phosphate + vinblastine sulfate/out
-
?
ATP + H2O + vincristine sulfate/in
-
Homo sapiens ADP + phosphate + vincristine sulfate/out
-
?
ATP + H2O + VP-16/in
-
Homo sapiens ADP + phosphate + VP-16/out
-
?
ATP + H2O + xenobiotic/in
-
Homo sapiens ADP + phosphate + xenobiotic/out
-
?

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens