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Literature summary for 7.6.2.2 extracted from

  • Zaja, R.; Loncar, J.; Popovic, M.; Smital, T.
    First characterization of fish P-glycoprotein (abcb1) substrate specificity using determinations of its ATPase activity and calcein-AM assay with PLHC-1/dox cell line (2011), Aquat. Toxicol., 103, 53-62.
    View publication on PubMed
Search for more literature for 7.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
nicardipine 1.9fold activation Poeciliopsis lucida
verapamil 1.8fold activation Poeciliopsis lucida

Inhibitors

Inhibitors Comment Organism Structure
2'-(4-ethoxyphenyl)-5-(4-methylpiperazin-1-yl)-1H,1'H-2,5'-bibenzo[d]imidazole almost complete inhibition of fish P-glycoprotein specific ATPase in micromolar concentrations Poeciliopsis lucida
cyclosporine A almost complete inhibition of fish P-glycoprotein specific ATPase in nanomolar concentrations Poeciliopsis lucida
PSC833 potent inhibitor in nanomolar concentrations, with some residual activity Poeciliopsis lucida

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.4
-
 ATP pH 7.0, 37°C Poeciliopsis lucida

Organism

Organism UniProt Comment Textmining
Poeciliopsis lucida
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
PLHC-1/dox cell fish hepatoma cells characterized by high overexpression of P-glycoprotein Poeciliopsis lucida
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + malachite green/in
-
 Poeciliopsis lucida ADP + phosphate + malachite green/out
-
 ?
additional information substrate comparison between fish P-glycoprotein and human P-glycoprotein, identification of five compounds that specifically interact only with fish P-glycoprotein, while seven compounds exhibit specific interaction only with human P-glycoprotein. Sixteen tested compounds show interaction with both proteins, and there is significant correlation in the interaction potency between fish and human P-glycoprotein for those compounds that interact with both proteins Poeciliopsis lucida ?
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 ?

Synonyms

Synonyms Comment Organism
ABCB1
-
 Poeciliopsis lucida
P-glycoprotein
-
 Poeciliopsis lucida

Expression

Organism Comment Expression
Poeciliopsis lucida high and specific P-glycoprotein transcript overexpression in PLHC-1/dox cells, about 160fold upregulation compared to PLHC-1/wt cells additional information