Literature summary for 7.6.2.2 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.

Search for more literature for 7.6.2.2

Cloned(Commentary)

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

Inhibitors

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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	gene ABCB1 encoding MDR1	-

Posttranslational Modification

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

Source Tissue

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

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 + rhodamine 123 /in	-	Homo sapiens	ADP + phosphate + rhodamine 123 /out	-	?
ATP + H2O + xenobiotic/in	-	Homo sapiens	ADP + phosphate + xenobiotic/out	-	?
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	-	?
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

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

Temperature Optimum [°C]

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

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

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Release 2023.1 (January 2023)