ABCB1 p.Met68Cys

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PMID: 12223492 [PubMed] Loo TW et al: "Location of the rhodamine-binding site in the human multidrug resistance P-glycoprotein."
No. Sentence Comment
130 The activity of M68C, was inhibited by 44%, whereas that of mutant L65C was increased (189%).
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ABCB1 p.Met68Cys 12223492:130:16
status: NEW
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PMID: 16042402 [PubMed] Loo TW et al: "ATP hydrolysis promotes interactions between the extracellular ends of transmembrane segments 1 and 11 of human multidrug resistance P-glycoprotein."
No. Sentence Comment
97 Figure 2A shows that the slower migrating product in mutants M68C(TM1)/Y950C(TM11), M68C- (TM1)/Y953C(TM11), M68C(TM1)/A954C(TM11), M69C- (TM1)/A954C(TM11), and M69C(TM1)/F957C(TM11) was greatly reduced upon exposure to 10 mM dithiothreitol.
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ABCB1 p.Met68Cys 16042402:97:84
status: NEW
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134 Membranes were prepared from HEK 293 cells (A), expressing mutants M68C(TM1)/Y950C(TM11), M68C(TM1)/Y953C(TM11), M68C- (TM1)/A954C(TM11), M69C(TM1)/A954C(TM11), M69C(TM1)/ F957C(TM11), or the negative mutant F72C(TM1)/F957C(TM11); (B) the single cysteine mutants M68C(TM1), M69C(TM1), Y950C(TM11), Y953C(TM11), A954C(TM11), or F957C(TM11); or (C) coexpressing the single cysteine mutants M68C(TM1) plus Y950C(TM11), M68C(TM1) plus Y953C(TM11), M68C(TM1) plus A954C(TM11), M69C(TM1) plus A954C(TM11), or M69C- (TM1) plus F957C(TM11).
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ABCB1 p.Met68Cys 16042402:134:113
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173 Histidine-tagged wild-type, Cys-less, and P-gp mutants M68C- (TM1)/Y950C(TM11), M68C(TM1)/Y953C(TM11), M68C(TM1)/ A954C(TM11), M69C(TM1)/A954C(TM11), or M69C(TM1)/ F957C(TM11) were expressed in HEK 293 cells.
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ABCB1 p.Met68Cys 16042402:173:55
status: NEW
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PMID: 16492138 [PubMed] Loo TW et al: "Transmembrane segment 1 of human P-glycoprotein contributes to the drug-binding pocket."
No. Sentence Comment
98 Verapamil Colchicine Vinblastine Mutant Vmax (%)* S50 (µM)† Vmax (%) S50 (µM) Vmax (%) S50 (µM) M51C 101 11.0 + - 0.6 96 391 + - 36 94 2.4 + - 0.2 V52C ND ND ND ND ND ND V53C 104 12.0 + - 0.2 101 389 + - 30 102 2.2 + - 0.1 G54C ND ND ND ND ND ND T55C 114 10.3 + - 1.1 95 418 + - 22 91 2.2 + - 0.1 L56C 103 12.2 + - 0.3 87 440 + - 41 95 2.5 + - 0.2 A57C 108 11.3 + - 0.3 98 377 + - 34 92 2.4 + - 0.2 A58C 90 12.5 + - 0.2 94 434 + - 20 95 2.6 + - 0.3 I59C 115 11.2 + - 0.8 95 380 + - 33 114 2.5 + - 0.2 I60C 102 11.1 + - 0.7 91 408 + - 18 110 2.5 + - 0.2 H61C 97 54.0 + - 5.0 61 912 + - 86 105 5.4 + - 0.4 G62C ND ND ND ND ND ND A63C 114 10.5 + - 1.2 99 362 + - 42 105 2.0 + - 0.3 G64C 106 45.0 + - 6.0 88 613 + - 55 60 2.4 + - 0.1 L65C 72 9.3 + - 1.1 112 368 + - 32 78 2.0 + - 0.2 P66C 95 13.0 + - 0.5 86 480 + - 39 97 2.8 + - 0.4 L67C 101 12.3 + - 0.3 106 423 + - 21 100 2.3 + - 0.1 M68C 119 9.7 + - 1.1 105 365 + - 32 92 2.3 + - 0.2 M69C 107 11.8 + - 0.6 110 431 + - 25 108 2.2 + - 0.1 L70C 94 11.4 + - 0.7 90 413 + - 18 98 2.3 + - 0.1 V71C 106 11.9 + - 0.3 90 370 + - 27 102 2.5 + - 0.5 Cys-less 100 12.0 + - 1.0 100 412 + - 48 100 2.2 + - 0.3 * Maximum activity relative to that of Cys-less P-gp.
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ABCB1 p.Met68Cys 16492138:98:905
status: NEW
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