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Literature summary extracted from

  • El-Readi, M.Z.; Hamdan, D.; Farrag, N.; El-Shazly, A.; Wink, M.
    Inhibition of P-glycoprotein activity by limonin and other secondary metabolites from Citrus species in human colon and leukaemia cell lines (2010), Eur. J. Pharmacol., 626, 139-145.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 beta-sitosterol-O-glucoside inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 deacetylnomilin inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 hesperidin inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 limonin inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 neohesperidin inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 stigmasterol inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents Homo sapiens
7.6.2.2 verapamil
-
Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 ATP + H2O + rhodamine 123/in Homo sapiens
-
ADP + phosphate + rhodamine 123/out
-
?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 Caco-2 cell
-
Homo sapiens
-
7.6.2.2 CEM-ADR5000 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + rhodamine 123/in
-
Homo sapiens ADP + phosphate + rhodamine 123/out
-
?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 MDR1
-
Homo sapiens
7.6.2.2 P-glycoprotein
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.6.2.2 0.134
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens beta-sitosterol-O-glucoside
7.6.2.2 0.169
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens neohesperidin
7.6.2.2 0.174
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens neohesperidin
7.6.2.2 0.195
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens hesperidin
7.6.2.2 0.21
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens stigmasterol
7.6.2.2 0.22
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens deacetylnomilin
7.6.2.2 0.23
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens hesperidin
7.6.2.2 0.285
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 Homo sapiens limonin
7.6.2.2 0.338
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens beta-sitosterol-O-glucoside
7.6.2.2 0.387
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens stigmasterol
7.6.2.2 0.478
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens deacetylnomilin
7.6.2.2 0.52
-
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells Homo sapiens limonin

General Information

EC Number General Information Comment Organism
7.6.2.2 physiological function mediates drug efflux from cells and plays a major role in causing multidrug resistance Homo sapiens