ABCB4 p.Tyr118Cys
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PMID: 11013259
[PubMed]
Loo TW et al: "Identification of residues within the drug-binding domain of the human multidrug resistance P-glycoprotein by cysteine-scanning mutagenesis and reaction with dibromobimane."
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183
DBBn also inhibited P-gp by reacting with cysteines in TM2 (Y118C and V125C) and TM8 (S766C).
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ABCB4 p.Tyr118Cys 11013259:183:60
status: NEW185 It is possible that some of these residues do not lie within the drug-binding site for these compounds because relatively high concentrations of dBBn were needed to inhibit 50% of the activity of mutants Y118C (TM2) and V125C (TM2) (740 and 870 M, respectively).
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ABCB4 p.Tyr118Cys 11013259:185:204
status: NEW186 Another possibility is that modification of mutant Y118C, V125C, or S766C blocks an essential conformational change during coupling of drug binding to ATPase activity.
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ABCB4 p.Tyr118Cys 11013259:186:51
status: NEW