ABCB1 p.Ile340Cys
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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.Ile340Cys 12223492:139:31
status: NEW155 Lower levels of protection were observed with mutants I340C, A841C, L975C, and V982C (Fig. 5).
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ABCB1 p.Ile340Cys 12223492:155:54
status: NEW
PMID: 14522974
[PubMed]
Loo TW et al: "Methanethiosulfonate derivatives of rhodamine and verapamil activate human P-glycoprotein at different sites."
No.
Sentence
Comment
150
It is interesting that residue F343C is on the same face of the TM6 ␣-helix as residue I340C (Fig. 6A).
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ABCB1 p.Ile340Cys 14522974:150:94
status: NEW151 Labeling of I340C with MTS-rhodamine, however, resulted in inhibition of ATPase activity (22).
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ABCB1 p.Ile340Cys 14522974:151:12
status: NEW152 Rhodamine B also protected I340C from labeling by MTS-rhodamine, indicating that this residue must be close to rhodamine-binding site.
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ABCB1 p.Ile340Cys 14522974:152:27
status: NEW154 Covalent modification of I340C may prevent P-gp from undergoing conformational changes during the transport cycle.
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ABCB1 p.Ile340Cys 14522974:154:25
status: NEW200 This may explain why both F343C and I340C can be labeled with MTS-rhodamine, but only F343C is activated upon labeling.
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ABCB1 p.Ile340Cys 14522974:200:36
status: NEW
PMID: 21991360
[PubMed]
Bikadi Z et al: "Predicting P-glycoprotein-mediated drug transport based on support vector machine and three-dimensional crystal structure of P-glycoprotein."
No.
Sentence
Comment
227
For example, activities of the human P-gp mutants, I340C (in TM6), L975C (in TM12), V981C (in TM12), and V982C (in TM12), were found to be highly protected from inhibition by MTS-rhodamine by pre-treatment with rhodamine B, indicating that these residues likely participate in rhodamine B binding to human P-gp [48].
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ABCB1 p.Ile340Cys 21991360:227:51
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.Ile340Cys 16545467:78:255
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.Ile340Cys 16545467:76:255
status: NEW