Literature summary for 7.6.2.2 extracted from

Collnot, E.M.; Baldes, C.; Wempe, M.F.; Kappl, R.; Huettermann, J.; Hyatt, J.A.; Edgar, K.J.; Schaefer, U.F.; Lehr, C.M.
Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity (2007), Mol. Pharmacol., 4(3), 465-474.

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Inhibitors

Inhibitors	Comment	Organism	Structure
D-alpha-tocopheryl polyethylene glycol 1000 succinate	i.e. TPGS 1000, water-soluble Vitamin E derivative. Inhibits substrate-induced ATPase activity without inducing significant ATPase activity on its own. Modulation of ATPase activity correlates with inhibitory potential for P-glycoprotein-mediated efflux	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
Caco-2 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + H2O	-	Homo sapiens	?	-	?

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0004	-	37°C, presence of nicardipine	Homo sapiens	D-alpha-tocopheryl polyethylene glycol 1000 succinate
0.00082	-	37°C, presence of quinidine	Homo sapiens	D-alpha-tocopheryl polyethylene glycol 1000 succinate
0.00318	-	37°C, presence of verapamil	Homo sapiens	D-alpha-tocopheryl polyethylene glycol 1000 succinate
0.00325	-	37°C, presence of progesterone	Homo sapiens	D-alpha-tocopheryl polyethylene glycol 1000 succinate

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Release 2023.1 (January 2023)