ABCB1 p.Phe804Ala
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PMID: 15530432
[PubMed]
Loo TW et al: "Thapsigargin or curcumin does not promote maturation of processing mutants of the ABC transporters, CFTR, and P-glycoprotein."
No.
Sentence
Comment
58
Mutations G251V and F804A are in the intracellular loops of the NH2- and COOH-terminal halves of P-gp, respectively.
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ABCB1 p.Phe804Ala 15530432:58:20
status: NEW70 Although the processing mutations (G251V, G300V, DY490, P709A, G722A, F804A, and P1194A) are located in different segments of P-gp, all the mutants could be rescued when expressed with drug substrates such as cyclosporin A.
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ABCB1 p.Phe804Ala 15530432:70:70
status: NEW90 We then compared the abilities of cyclosporin A, thapsigargin, and curcumin to induce maturation of P-gp processing mutants G251V, G300V, DY490, P709A, G722A, F804A, and P1194A.
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ABCB1 p.Phe804Ala 15530432:90:159
status: NEW
PMID: 24275649
[PubMed]
Loo TW et al: "Locking intracellular helices 2 and 3 together inactivates human P-glycoprotein."
No.
Sentence
Comment
79
It was Clamping IH2 to IH3 Inhibits P-gp 230 JOURNAL OF BIOLOGICAL CHEMISTRY VOLUME 289ߦNUMBER 1ߦJANUARY 3, found that two mutations in IH3 (W803A and F804A) inhibited maturation of P-gp (Fig. 1, B and C) so that immature 150-kDa P-gp was the major product.
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ABCB1 p.Phe804Ala 24275649:79:165
status: NEW83 Because W803A and F804A mutations in IH3 yielded the immature 150-kDa immature P-gp as the major product, we tested whether the mutants could be rescued with cyclosporine A.
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ABCB1 p.Phe804Ala 24275649:83:18
status: NEW85 Accordingly, the A52-tagged mutants W803A and F804A were expressed in HEK 293 cells in the absence or presence of 5 òe;M cyclosporine A, and whole cell SDS extracts were subjected to immunoblot analysis. Fig. 2A shows that expression of either W803A or F804A in the presence of cyclosporine A yielded the mature 170-kDa P-gp as the major product.
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ABCB1 p.Phe804Ala 24275649:85:46
status: NEWX
ABCB1 p.Phe804Ala 24275649:85:257
status: NEW89 To determine whether the W803A and F804A mutants rescued with cyclosporine A were active, the histidine-tagged mutants W803A and F804A were expressed in HEK 293 cells in the presence of cyclosporine A, and P-gp was isolated by nickel-chelate chromatography.
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ABCB1 p.Phe804Ala 24275649:89:35
status: NEWX
ABCB1 p.Phe804Ala 24275649:89:129
status: NEW101 Drug rescue of processing mutants and activity of IH3 mutants W803A and F804A.
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ABCB1 p.Phe804Ala 24275649:101:72
status: NEW102 A52-tagged WT P-gp, mutants W803A and F804A (A), or IH3 flanking mutants (F793A, L797A, L814A, and L818A) (B) were expressed in HEK293cellsintheabsence(afa;)orpresence(af9;)of5òe;M cyclosporineA(Cyclo) for 18 h, and whole cell extracts were subjected to immunoblot analysis.
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ABCB1 p.Phe804Ala 24275649:102:38
status: NEW103 The positions of mature (170-kDa) and immature (150-kDa) forms of P-gp are shown. C, verapamil-stimulated ATPase activities of histidine-tagged wild-type P-gp and W803A and F804A mutants.
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ABCB1 p.Phe804Ala 24275649:103:173
status: NEW109 Mutating Phe804 to Leu, Ser, or Asp inhibited maturation, and only the F804A or F804S mutants could be rescued with cyclosporine A to yield mature 170-kDa P-gp as the major product (Fig. 3, C and D).
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ABCB1 p.Phe804Ala 24275649:109:71
status: NEW