Literature summary for 7.6.2.2 extracted from

Nabekura, T.; Yamaki, T.; Ueno, K.; Kitagawa, S.
Effects of plant sterols on human multidrug transporters ABCB1 and ABCC1 (2008), Biochem. Biophys. Res. Commun., 369, 363-368.

Search for more literature for 7.6.2.2

Activating Compound

Activating Compound	Comment	Organism	Structure
trans,trans-4,17(20)-pregnadiene-3,16-dione	i.e. z-guggulsterone, stimulation of ATPase activity, inhibitory to substrate transport	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
overexpression of both isoforms ABCB1 and ABCC1 in KB-C2 and KB/MRP cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
trans,trans-4,17(20)-pregnadiene-3,16-dione	i.e. Z-guggulsterone. In presence of guggulsterone, fluorescent substrates daunorubicin or rhodamine 123 accumulate in KB-C2 cells. Efflux of rhodamine 123 is inhibited and the accumulation of substrate calcein is increased. ATPase activities of both isoforms ABCB1 And ABCC1 are stimulated	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isoforms ABCB1 and ABCC1	-

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Release 2023.1 (January 2023)