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PMID: 14598019
Gerloff T
Impact of genetic polymorphisms in transmembrane carrier-systems on drug and xenobiotic distribution.
Naunyn Schmiedebergs Arch Pharmacol. 2004 Jan;369(1):69-77. Epub 2003 Nov 4.,
[PubMed]
Sentences
No.
Mutations
Sentence
Comment
145
ABCB1 p.Gly1249Ala
X
ABCB1 p.Gly1249Ala 14598019:145:91
status:
NEW
view ABCB1 p.Gly1249Ala details
Frequently occurring SNPs were C24T (18.8%) of the promoter region and the two exonic SNPs
G1249A
(12.5%, exon 10) and C3972T (21.9%, exon 28).
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166
ABCC1 p.Arg433Ser
X
ABCC1 p.Arg433Ser 14598019:166:156
status:
NEW
view ABCC1 p.Arg433Ser details
Digoxin plasma levels are inversely correlated with Pgp expression levels The functional relevance of the MRP1 SNPs G671 V, positioned within NBD1, and of
Arg433Ser
, located in a putative cytoplasmic loop, was tested using in vitro transport assays (Conrad et al. 2002).
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167
ABCC1 p.Arg433Ser
X
ABCC1 p.Arg433Ser 14598019:167:90
status:
NEW
view ABCC1 p.Arg433Ser details
While the first did not change MRP1 transport activity for conjugated organic anions, the
Arg433Ser
polymorphism reduced transport activity of the substrates leucotriene C4 and estrone sulfate by half due to a decrease in Vmax for both compounds, whereas Km remained unchanged.
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168
ABCC1 p.Arg433Ser
X
ABCC1 p.Arg433Ser 14598019:168:71
status:
NEW
view ABCC1 p.Arg433Ser details
In addition, doxorubicin-resistance of cells overexpressing the mutant
Arg433Ser
MRP1 was 2-fold higher compared to the wild-type.
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