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Literature summary for 7.6.2.2 extracted from

  • Ohnuma, S.; Chufan, E.; Nandigama, K.; Jenkins, L.M.; Durell, S.R.; Appella, E.; Sauna, Z.E.; Ambudkar, S.V.
    Inhibition of multidrug resistance-linked P-glycoprotein (ABCB1) function by 5-fluorosulfonylbenzoyl 5-adenosine: evidence for an ATP analogue that interacts with both drug-substrate-and nucleotide-binding sites (2011), Biochemistry, 50, 3724-3735.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expression in High Five insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5'-O-[4-(fluorosulfonyl)benzoyl]adenosine incubation inhibits ATP hydrolysis and the binding of 8-azido-ATP. 5'-Fluorosulfonylbenzoyl 5'-adenosine is an ATP analog that interacts with both the drug-binding and ATP-binding sites of P-gp, but fluorosulfonyl-mediated crosslinking is observed only at the nucleotide-binding domains Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
KB-3-1 cell
-
 Homo sapiens
-
KB-V1 cell overexpression of P-gp Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.21
-
 hydrolysis of ATP, pH 7.5, 37°C Homo sapiens 5'-O-[4-(fluorosulfonyl)benzoyl]adenosine
0.68
-
 binding of 8-azido-ATP, pH 7.5, 37°C Homo sapiens 5'-O-[4-(fluorosulfonyl)benzoyl]adenosine