ABCB1 p.Phe804Asp
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PMID: 25456855
[PubMed]
Loo TW et al: "Tariquidar inhibits P-glycoprotein drug efflux but activates ATPase activity by blocking transition to an open conformation."
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Sentence
Comment
28
Only tariquidar promoted maturation of misprocessed mutant F804D to yield mature P-gp.
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ABCB1 p.Phe804Asp 25456855:28:59
status: NEW68 After 5 h at 37 8C, the medium was replaced with fresh medium with or without 5 mM cyclosporine A or 0.5 mM tariquidar for rescue of mutant F804D and 500 nM tariquidar, 10 mM cyclosporine A, 50 mM verapamil, 20 mM vinblastine or 100 mM capsaicin for rescue of TMD1+2.
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ABCB1 p.Phe804Asp 25456855:68:140
status: NEW185 We previously found that some P-gp mutants such as F804D could not be rescued by any drug substrate [45].
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ABCB1 p.Phe804Asp 25456855:185:51
status: NEW186 The F804D mutation is located in intracellular helix 3 that mediates contact between the third intracellular loop (ICL3) in TMD2 and NBD1.
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ABCB1 p.Phe804Asp 25456855:186:4
status: NEW187 To test if tariquidar could promote maturation of F804D, the A52-tagged mutant was transiently expressed in the presence of 300 nM of the compound for 18 h.
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ABCB1 p.Phe804Asp 25456855:187:50
status: NEW188 Immunoblot analysis of whole cell SDS extracts showed that tariquidar could promote maturation of F804D to yield mature P-gp as about 50% of the steady-state product (Fig. 4C and D).
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ABCB1 p.Phe804Asp 25456855:188:98
status: NEW208 Does tariquidar also inhibit A80C/R741C cross-linking when A B G268V 0 12.5 25 50 100 200 400 800 [Tar] (nM) 170 kDa 150 kDa GAPDH C D 170 kDa 150 kDa GAPDH None Cyclo Tariq F804D 0 20 40 60 80 100 Percent Mature [Tariq] nM 0 12.5 25 50 100 200 400 800 * * * * * * None Cyclo Tariq 0 20 40 60 80 100 Percent Mature * Fig. 4.
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ABCB1 p.Phe804Asp 25456855:208:174
status: NEW215 (C) Whole cell extracts of HEK 293 cells expressing A52-tagged P-gp processing mutant F804D in the absence (None) or presence of 10 mM cyclosporine A (Cyclo) or 300 nM tariquidar (Tariq) were subjected to immunoblot analysis.
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ABCB1 p.Phe804Asp 25456855:215:86
status: NEW306 Perhaps tariquidar acts as a particularly effective pharmacological chaperone to rescue P-gp processing mutants such as F804D (Fig. 4C) because it interacts at both the predicted Rand H-sites to have an additive effect on maturation.
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ABCB1 p.Phe804Asp 25456855:306:120
status: NEW
PMID: 25987565
[PubMed]
Loo TW et al: "The Transmission Interfaces Contribute Asymmetrically to the Assembly and Activity of Human P-glycoprotein."
No.
Sentence
Comment
159
For example, tariquidar but not cyclosporine A could repair the F804D mutation at the ICL3-NBD1 interface (41).
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ABCB1 p.Phe804Asp 25987565:159:64
status: NEW