Literature summary for 7.6.2.2 extracted from

Bessadok, A.; Garcia, E.; Jacquet, H.; Martin, S.; Garrigues, A.; Loiseau, N.; Andre, F.; Orlowski, S.; Vivaudou, M.
Recognition of sulfonylurea receptor (ABCC8/9) ligands by the multidrug resistance transporter P-glycoprotein (ABCB1): functional similarities based on common structural features between two multispecific ABC proteins (2011), J. Biol. Chem., 286, 3552-3569.

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Activating Compound

Activating Compound	Comment	Organism	Structure
Diazoxide	about 55% increase in ATPase activity, half-activation concentration is 0.6 mM	Cricetulus griseus
glibenclamide	augments the ATPase activity with a maximum attained near 100 microM	Cricetulus griseus
meglitinide	increases ATPase activity, maximum activation levels of 70%	Cricetulus griseus
additional information	ligands of sulfonylurea receptor SUR also interact with P-plycoprotein, due to structural similarity between drug binding domains in the two proteins	Cricetulus griseus
P1075	about 55% increase in ATPase activity, half-activation concentration is 0.036 mM	Cricetulus griseus
SR47063	100% increase in ATPase activity, half-activation concentration is 1.5 mM	Cricetulus griseus
Tolbutamide	increases ATPase activity, with maximum activation levels of 70%	Cricetulus griseus

Organism

Organism	UniProt	Comment	Textmining
Cricetulus griseus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
DC-3F/ADX cell	selected from spontaneously transformed Chinese hamster lung fibroblast DC-3F on the basis of resistance to actinomycin D	Cricetulus griseus	-

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Release 2023.1 (January 2023)