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Literature summary extracted from

  • Molnar, J.; Kars, M.D.; Guenduez, U.; Engi, H.; Schumacher, U.; Van Damme, E.J.; Peumans, W.J.; Makovitzky, J.; Gyemant, N.; Molnar, P.
    Interaction of tomato lectin with ABC transporter in cancer cells: Glycosylation confers functional conformation of P-gp (2009), Acta Histochem., 111, 329-333.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 gene ABCB1 maps to chromosome 7q21.1, expression of MDR1 in L5178 mouse T-cell lymphoma cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 10-(3-(dimethylamino)propyl)-2-(trifluoromethyl)phenothiazine
-
 Homo sapiens
7.6.2.2 Promethazine
-
 Homo sapiens
7.6.2.2 semi-beta-carotene-epoxide
-
 Homo sapiens
7.6.2.2 tomato lectin
-
 Homo sapiens
7.6.2.2 verapamil
-
 Homo sapiens

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 + xenobiotic/in Homo sapiens P-gp 170 has two potentially interesting regions for drugs interfering with its efflux function, namely the oligosaccharides on the first extracellular loop with unknown function and the two intracellular ATP-binding regions providing the energy for drug efflux function. P-gp is a polytopic plasma membrane protein whose overexpression causes multidrug resistance, MDR, responsible for the failure of cancer chemotherapy ADP + phosphate + xenobiotic/out
-
 ?
7.6.2.2 additional information Homo sapiens The polylactoseamine oligosaccharides on the first loop of P-gp 170 can specifically bind the tomato lectin which possibly stabilizes the functional active conformation of P-gp ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
 gene ABCB1 encoding MDR1
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
7.6.2.2 glycoprotein P-gp is a highly glycosylated plasma membrane protein that exists in several glycoforms, with different degrees of glycosylation Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 brain
-
 Homo sapiens
-
7.6.2.2 brain capillary endothelial cell line
-
 Homo sapiens
-
7.6.2.2 colonic epithelium
-
 Homo sapiens
-
7.6.2.2 hepatocyte
-
 Homo sapiens
-
7.6.2.2 pancreas
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
7.6.2.2 additional information
-
-
 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
-
 ?
7.6.2.2 ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
7.6.2.2 ATP + H2O + xenobiotic/in P-gp 170 has two potentially interesting regions for drugs interfering with its efflux function, namely the oligosaccharides on the first extracellular loop with unknown function and the two intracellular ATP-binding regions providing the energy for drug efflux function. P-gp is a polytopic plasma membrane protein whose overexpression causes multidrug resistance, MDR, responsible for the failure of cancer chemotherapy Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
7.6.2.2 additional information The polylactoseamine oligosaccharides on the first loop of P-gp 170 can specifically bind the tomato lectin which possibly stabilizes the functional active conformation of P-gp Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
 Homo sapiens
7.6.2.2 MDR1
-
 Homo sapiens
7.6.2.2 More P-gp 170 is a member of the ATP-binding cassette, ABC, transporter superfamily Homo sapiens
7.6.2.2 P-gp
-
 Homo sapiens
7.6.2.2 PGY1
-
 Homo sapiens
7.6.2.2 phospho-glycoprotein
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.6.2.2 37
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
7.6.2.2 ATP
-
 Homo sapiens