ABCB1 p.Ala342Cys
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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
139
The activities of two mutants (I340C and A342C) in TM6 were strongly inhibited (87 and 94%, respectively) by MTS-rhodamine.
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ABCB1 p.Ala342Cys 12223492:139:41
status: NEW
PMID: 9405384
[PubMed]
Loo TW et al: "Identification of residues in the drug-binding site of human P-glycoprotein using a thiol-reactive substrate."
No.
Sentence
Comment
21
We show that the drug-stimulated ATPase activities of mutants L339C and A342C (TM6) and L975C, V982C, and A985C (TM12) were particularly sensitive to inhibition by dBBn and that the inhibition was prevented by various drug substrates.
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ABCB1 p.Ala342Cys 9405384:21:72
status: NEW83 There was no detectable activity with mutants S344C, G341C, and G984C, whereas mutants A342C, G346C, Q347C, A985C, G989C, and Q990C had much reduced activity (10-40%).
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ABCB1 p.Ala342Cys 9405384:83:87
status: NEW89 Mutants A342C and Q347C also showed enhanced degradation in the absence of cyclosporin A, with the 120-kDa protein as the major product.
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ABCB1 p.Ala342Cys 9405384:89:8
status: NEW98 In contrast, mutants L339C, A342C, L975C, V982C, and A985C were significantly inhibited by dBBn, because they retained only 10, 40, 13, 25, and 32% of their activities, respectively.
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ABCB1 p.Ala342Cys 9405384:98:28
status: NEW99 The concentration of dBBn required to give 50% inhibition of ATPase activity for mutants L339C, L975C, V982C, A985C, and A342C were 90, 112, 320, 480, and 700 M, respectively.
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ABCB1 p.Ala342Cys 9405384:99:121
status: NEW111 The P-glycoproteins(His)10 of Cys-less and mutants L339C, A342C, L975C, V982C, and A985C were mixed with lipid and then preincubated for 15 min at 4 °C without drug or in the presence of 2 mM verapamil (Ver.
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ABCB1 p.Ala342Cys 9405384:111:58
status: NEW114 Mutants A342C and A985C were preincubated with verapamil only.
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ABCB1 p.Ala342Cys 9405384:114:8
status: NEW121 Due to the low ATPase activities of mutants A342C and A985C, their protection assays were done only in the presence of verapamil.
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ABCB1 p.Ala342Cys 9405384:121:44
status: NEW123 As shown in Fig. 4, mutants A342C and A985C were protected from dBBn inactivation by verapamil.
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ABCB1 p.Ala342Cys 9405384:123:28
status: NEW
PMID: 16545467
[PubMed]
Shilling RA et al: "New light on multidrug binding by an ATP-binding-cassette transporter."
No.
Sentence
Comment
78
Single-cysteine mutants in human P-glycoprotein that are protected from cross-linking to cysteine-reactive MTS substrate analogues by the non-reactive substratea P-glycoprotein residueb Corresponding residue in V. cholera MsbA Cysteine-reactive substrate I340C (6) G293 MTS-rhodamine A841C (9) A151 MTS-rhodamine L975C (12) T285 MTS-rhodamine V981C (12) M291 MTS-rhodamine V982C (12) F292 MTS-rhodamine S222C (4) A175 MTS-verapamil L339C (6) M291 MTS-verapamil A342C (6) M295 MTS-verapamil I868C (10) F180 MTS-verapamil F942C (11) Q256 MTS-verapamil T945C (11) A259 MTS-verapamil G984C (12) L294 MTS-verapamil a Data adapted from [24,2].
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ABCB1 p.Ala342Cys 16545467:78:461
status: NEW76 Single-cysteine mutants in human P-glycoprotein that are protected from cross-linking to cysteine-reactive MTS substrate analogues by the non-reactive substratea P-glycoprotein residueb Corresponding residue in V. cholera MsbA Cysteine-reactive substrate I340C (6) G293 MTS-rhodamine A841C (9) A151 MTS-rhodamine L975C (12) T285 MTS-rhodamine V981C (12) M291 MTS-rhodamine V982C (12) F292 MTS-rhodamine S222C (4) A175 MTS-verapamil L339C (6) M291 MTS-verapamil A342C (6) M295 MTS-verapamil I868C (10) F180 MTS-verapamil F942C (11) Q256 MTS-verapamil T945C (11) A259 MTS-verapamil G984C (12) L294 MTS-verapamil a Data adapted from [24,25].
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ABCB1 p.Ala342Cys 16545467:76:461
status: NEW