Literature summary for 7.6.2.1 extracted from

Morita, S.Y.; Kobayashi, A.; Takanezawa, Y.; Kioka, N.; Handa, T.; Arai, H.; Matsuo, M.; Ueda, K.
Bile salt-dependent efflux of cellular phospholipids mediated by ATP binding cassette protein B4 (2007), Hepatology, 46, 188-199.

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Activating Compound

Activating Compound	Comment	Organism	Structure
cholate	slightly increases the efflux of phospholipids and cholesterol from cells	Homo sapiens
glycocholate	slightly increases the efflux of phospholipids and cholesterol from cells	Homo sapiens
additional information	effects of bile salt structure on ABCB4-mediated lipid secretion, overview	Homo sapiens
taurocholate	increases the efflux of phospholipids and cholesterol from cells, the taurocholate monomer plays an important role in ABCB4-mediated lipid secretion	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
stable expression of ABCB4 in HEK-293 cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
K1075M	site-directed mutagenesis in the Walker A motif results in an inactive mutant	Homo sapiens
K435M	site-directed mutagenesis in the Walker A motif results in an inactive mutant	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
verapamil	complete inhibition at 0.05 mM	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
plasma membrane	-	Homo sapiens	5886	-

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da]	Molecular Weight Maximum [Da]	Comment	Organism
140000	-	x * 140000, recombinant ABCB4, SDS-PAGE	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + H2O + phosphatidylserine/in	Homo sapiens	ABCB4 mediates the efflux of phospholipids into the canalicular lumen in the presence of bile salts, and plays a crucial role in bile formation and lipid homeostasis	ADP + phosphate + phosphatidylserine/out	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
glycoprotein	analysis of glycosylation of ABCB4, cleavage by endoglycosidase H or peptide N-glycosidase F, overview	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
hepatocyte	canalicular membrane	Homo sapiens	-
additional information	no endogenous ABCB4 activity in HEK-293 cells	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + H2O + phosphatidylserine/in	ABCB4 mediates the efflux of phospholipids into the canalicular lumen in the presence of bile salts, and plays a crucial role in bile formation and lipid homeostasis	Homo sapiens	ADP + phosphate + phosphatidylserine/out	-	?
ATP + H2O + phosphatidylserine/in	ABCB4 is required for ATP-dependent phosphatidylcholine secretion into the bile and to translocate phosphatidylcholine across the plasma membrane, overview	Homo sapiens	ADP + phosphate + phosphatidylserine/out	-	?

Subunits

Subunits	Comment	Organism
?	x * 140000, recombinant ABCB4, SDS-PAGE	Homo sapiens

Synonyms

Synonyms	Comment	Organism
ABCB4	-	Homo sapiens
MDR3 P-glycoprotein	-	Homo sapiens
More	cf. EC 3.6.3.44	Homo sapiens
multidrug resistance 3 P-glycoprotein	-	Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	assay at	Homo sapiens

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Release 2023.1 (January 2023)