ABCMdb

ABCB1 p.Phe957Ala

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Publications

PMID: 10585407 [PubMed] Loo TW et al: "Identification of residues in the drug-binding domain of human P-glycoprotein. Analysis of transmembrane segment 11 by cysteine-scanning mutagenesis and inhibition by dibromobimane."

No. Sentence Comment

77 There was moderate stimulation of verapamil-stimulated ATPase activities in mutants T945A (140%), G955V (143%), and F957A (126%). Login to comment
84 Moderate decreases in activity (40-50%) were observed for mutants G939V, Q946A, A947L, Y953A, and F957A. Login to comment
100 There were, however, significant decreases in the activity for mutants Q946A (18%), F942A (24%), and F957A (32%). Login to comment
128 TABLE I Drug-stimulated ATPase activity Mutant Drug Verapamil Vinblastine Colchicine Vmax Km Vmax Km Vmax Km % of WTa ␮M % of WT ␮M % of WT mM WT 100 24 100 5.4 100 0.62 I937S 94 22 93 6.1 100 0.69 F938A 106 32 96 5.1 96 0.68 G939V 62 8 45 4.0 165 0.26 I940S 93 32 93 5.6 93 0.65 T941A 100 25 104 5.5 100 0.66 F942A 88 93 30 5.1 24 0.80 S943A 92 26 100 5.2 85 0.62 F944A 93 14 105 5.3 101 0.64 T945A 140 100 165 8.3 56 0.65 Q946A 101 165 57 8.5 18 0.64 A947L 105 156 60 13.0 51 1.87 M948A 103 23 101 5.9 103 0.62 M949A 82 40 96 5.5 61 0.60 Y950A 109 37 119 5.1 99 0.62 F951A 94 31 99 5.2 101 0.64 S952A 108 36 123 5.1 91 0.69 Y953A 205 110 59 8.5 131 0.67 A954L 108 44 13 NDb 8 ND G955V 143 10 104 3.5 220 0.47 C956A 97 24 95 5.3 145 0.63 F957A 126 21 47 4.8 32 1.0 a WT, wild type. b ND, not determined due to low activity. Login to comment

PMID: 8639515 [PubMed] Hanna M et al: "Mutagenesis of transmembrane domain 11 of P-glycoprotein by alanine scanning."

No. Sentence Comment

239 In previous work (Loo & Clarke, 1993b), the same mutation was made in the same residue at the equivalent position in P-gp encoded by the human MDR1 isoform (F957A). Login to comment