ABCB4 p.Phe728Cys
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PMID: 17636884
[PubMed]
Loo TW et al: "Nucleotide binding, ATP hydrolysis, and mutation of the catalytic carboxylates of human P-glycoprotein cause distinct conformational changes in the transmembrane segments."
No.
Sentence
Comment
74
The positions of the catalytic carboxylate mutations (E556Q in NBD1 and E1201Q in NBD2) and the cysteine mutations in the TM segments used in the disulfide cross-linking studies (L332C, L339C, F343C, F728C, L975C, and V982C) are shown.
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ABCB4 p.Phe728Cys 17636884:74:200
status: NEW146 Samples were then subjected to immunoblot analysis. Figure 5C shows that in the absence of vinblastine, almost all of the mutant L339C(TM6)/F728C- (TM7) P-gp was cross-linked in the presence of ADP or ATP.
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ABCB4 p.Phe728Cys 17636884:146:140
status: NEW149 In contrast, the cross-linking efficiency of mutant L339C(TM6)/F728C- (TM7) in the absence of vinblastine was reduced in the presence of AMP‚PNP.
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ABCB4 p.Phe728Cys 17636884:149:63
status: NEW156 To further inhibit the ATPase activity of mutant L339C(TM6)/F728C- (TM7), the E556Q(NBD1) and E1201Q(NBD2) catalytic carboxylate mutations were introduced.
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ABCB4 p.Phe728Cys 17636884:156:60
status: NEW192 Cross-linking of mutant L339C(TM6)/F728C- (TM7) (Figure 6) was observed to be ~4-fold faster in the presence of ATP than in the presence of AMP‚PNP.
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ABCB4 p.Phe728Cys 17636884:192:35
status: NEW245 In contrast, we did not observe any detectable difference in the apparent affinity for vinblastine in the presence of ATP (Figures 6 and 7) during cross-linking of mutant L339C(TM6)/F728C- (TM7).
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ABCB4 p.Phe728Cys 17636884:245:182
status: NEW
PMID: 22700974
[PubMed]
Loo TW et al: "The ATPase activity of the P-glycoprotein drug pump is highly activated when the N-terminal and central regions of the nucleotide-binding domains are linked closely together."
No.
Sentence
Comment
254
For example, covalent labeling of F728C (TM7) (22), L65C (TM1) (57), or I306C (TM5) (24) with a thiol-reactive derivative of verapamil increased basal ATPase activity of P-gp by 7-12-fold.
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ABCB4 p.Phe728Cys 22700974:254:34
status: NEW247 For example, covalent labeling of F728C (TM7) (22), L65C (TM1) (57), or I306C (TM5) (24) with a thiol-reactive derivative of verapamil increased basal ATPase activity of P-gp by 7-12-fold.
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ABCB4 p.Phe728Cys 22700974:247:34
status: NEW