ABCB1 p.Tyr1087Leu
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PMID: 24275649
[PubMed]
Loo TW et al: "Locking intracellular helices 2 and 3 together inactivates human P-glycoprotein."
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Comment
11
Mutants Y1087A and Y1087L, but not Y1087F, were misprocessed, and all inhibited ATPase activity.
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ABCB1 p.Tyr1087Leu 24275649:11:19
status: NEW148 To test whether Tyr1087 was important for folding or mediating drug stimulation of ATPase activity, we tested the effect of Y1087A, Y1087L, and Y1087F mutations.
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ABCB1 p.Tyr1087Leu 24275649:148:132
status: NEW149 The A52-tagged mutants were expressed in HEK 293 cells in the absence or presence of cyclosporine A, and samples of whole cell SDS extracts were subjected to immunoblot analysis. Fig. 5A shows that the mature 170-kDa protein was the major product in mutant Y1087F, whereas the 150-kDa immature protein was the major product in mutants Y1087A and Y1087L.
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ABCB1 p.Tyr1087Leu 24275649:149:346
status: NEW150 Both mutants Y1087A and Y1087L, however, could be rescued when they were expressed in the presence of cyclosporine A (Fig. 5A).
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ABCB1 p.Tyr1087Leu 24275649:150:24
status: NEW153 It was found that the Y1087A and Y1087L mutations reduced activity by over 90% (Fig. 5B).
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ABCB1 p.Tyr1087Leu 24275649:153:33
status: NEW164 A, A52-tagged Y1087A (A), Y1087F (F), and Y1087L (L) mutants were expressed in the absence (afa;) or presence (af9;) of 5 òe;M cyclosporine A (Cyclo).
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ABCB1 p.Tyr1087Leu 24275649:164:42
status: NEW166 The positions of mature (170-kDa) and immature (150-kDa) P-gps are indicated. B, histidine-tagged WT, Y1087A (A), Y1087F (F), and Y1087L (L) P-gp were expressed in HEK 293 cells and isolated by nickel-chelate chromatography.
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ABCB1 p.Tyr1087Leu 24275649:166:130
status: NEW167 Mutants Y1087A and Y1087L were expressed in the presence of cyclosporine A to promote maturation.
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ABCB1 p.Tyr1087Leu 24275649:167:19
status: NEW171 Mutations of Tyr1087 to Ala or Leu severely reduced both maturation and activity of P-gp, and even the small change of replacing Tyr with Phe caused about a 70% reduction in activity.
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ABCB1 p.Tyr1087Leu 24275649:171:13
status: NEW203 Mutation of Tyr1087 to Leu severely inhibited activity, whereas the conservative Y1087F change caused about a 70% reduction in activity.
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ABCB1 p.Tyr1087Leu 24275649:203:12
status: NEW