ABCB1 p.Ile297Arg
| Predicted by SNAP2: | A: N (66%), C: N (66%), D: D (85%), E: D (80%), F: N (87%), G: D (71%), H: D (75%), K: D (80%), L: N (93%), M: N (82%), N: D (80%), P: D (85%), Q: D (75%), R: D (80%), S: D (63%), T: N (61%), V: N (87%), W: D (63%), Y: D (71%), |
| Predicted by PROVEAN: | A: D, C: D, D: D, E: D, F: N, G: D, H: D, K: D, L: N, M: N, N: D, P: D, Q: D, R: D, S: D, T: D, V: N, W: D, Y: D, |
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[hide] Drug rescue distinguishes between different struct... Biochemistry. 2013 Oct 15;52(41):7167-9. doi: 10.1021/bi401269m. Epub 2013 Oct 2. Loo TW, Clarke DM
Drug rescue distinguishes between different structural models of human P-glycoprotein.
Biochemistry. 2013 Oct 15;52(41):7167-9. doi: 10.1021/bi401269m. Epub 2013 Oct 2., [PMID:24083983]
Abstract [show]
There is no high-resolution crystal structure of the human P-glycoprotein (P-gp) drug pump. Homology models of human P-gp based on the crystal structures of mouse or Caenorhabditis elegans P-gps show large differences in the orientation of transmembrane segment 5 (TM5). TM5 is one of the most important transmembrane segments involved in drug-substrate interactions. Drug rescue of P-gp processing mutants containing an arginine at each position in TM5 was used to identify positions facing the lipid or internal aqueous chamber. Only the model based on the C. elegans P-gp structure was compatible with the drug rescue results.
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No. Sentence Comment
27 Examples of drug rescue of G251V and TM5 mutants G251V/I297R and G251V/S298R are shown in Figure 1B. When processing mutant G251V is expressed in the absence of cyclosporine A, the major product was the immature 150 kDa protein (~95% of total P-gp).
X
ABCB1 p.Ile297Arg 24083983:27:55
status: NEW29 Mutant S298R but not I297R could be rescued by cyclosporine A.
X
ABCB1 p.Ile297Arg 24083983:29:21
status: NEW