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Literature summary for 7.6.2.2 extracted from

  • Wan, C.K.; Zhu, G.Y.; Shen, X.L.; Chattopadhyay, A.; Dey, S.; Fong, W.F.
    Gomisin A alters substrate interaction and reverses P-glycoprotein-mediated multidrug resistance in HepG2-DR cells (2006), Biochem. Pharmacol., 72, 824-837.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
overexpression in Hep-G2 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
gomisin A strongly inhibits P-glycoprotein ATPase activity in cells overexpressing the enzyme. Alters substrate interaction of P-glycoprotein but itself is neither a substrate nor a competitive inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00271
-
 verapamil/in presence of 0.4 mM gomisin A, pH 7.4, 37°C Homo sapiens
0.00426
-
 progesterone/in presence of 0.4 mM gomisin A, pH 7.4, 37°C Homo sapiens
0.00515
-
 verapamil/in pH 7.4, 37°C Homo sapiens
0.00553
-
 verapamil/in presence of 0.04 mM gomisin A, pH 7.4, 37°C Homo sapiens
0.01
-
 progesterone/in presence of 0.04 mM gomisin A, pH 7.4, 37°C Homo sapiens
0.0194
-
 progesterone/in pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + progesterone/in
-
 Homo sapiens ADP + phosphate + progesterone/out
-
 ?
ATP + H2O + verapamil/in
-
 Homo sapiens ADP + phosphate + verapamil/out
-
 ?