ABCMdb

PMID: 21175590

Kerr ID, Haider AJ, Gelissen IC
The ABCG family of membrane-associated transporters: you don't have to be big to be mighty.
Br J Pharmacol. 2010 Dec 22. doi: 10.1111/j.1476-5381.2010.01177.x., 2010-12-22 [PubMed]

Sentences

No. Mutations Sentence Comment

33 ABCG2 p.Arg482Gly Although performed with a mutant isoform of ABCG2 (Arg482Gly) this study remains the only direct determination of substrate binding affinities in a human ABCG transporter. Login to comment 38 ABCG2 p.Arg482Gly Prazosin displayed much lower potency whilst methotrexate (which is not transported by the R482G isoform) was unable to displace the bound radioligand (Clark et al., 2006). Login to comment 51 ABCG2 p.Arg482Gly Although performed with a mutant isoform of ABCG2 (Arg482Gly) this study remains the only direct determination of substrate binding affinities in a human ABCG transporter. Login to comment 56 ABCG2 p.Arg482Gly Prazosin displayed much lower potency while methotrexate (which is not transported by the R482G isoform) was unable to displace the bound radioligand (Clark et al., 2006). Login to comment 143 ABCG2 p.Gln141Lys The effects in vivo are rather less well understood, with the exception of the SNP rs2231142 (resulting in a Gln141Lys change). Login to comment 145 ABCG2 p.Gln141Lys Interestingly, previous analysis had suggested that the Gln141Lys variant of ABCG2 was only subtly different in terms of export of chemotherapeutic drugs compared to wild type ABCG2 (Tamura et al., 2007), which emphasises that studies on the impact of SNPs on ABCG2 function have to be taken into the context of the extreme diversity of transport substrates. Login to comment 150 ABCG5 p.Arg50Cys The former identified a single locus effect of SNP rs4245791 (in intron 3 of the ABCG8) on total cholesterol levels, whilst the latter identified rs6756629 (resulting in an Arg50Cys change in ABCG5) as being associated with both raised total and LDL‐cholesterol. Login to comment 167 ABCG2 p.Gln141Lys The effects in vivo are rather less well understood, with the exception of the SNP rs2231142 (resulting in a Gln141Lys change). Login to comment 169 ABCG2 p.Gln141Lys Interestingly, previous analysis had suggested that the Gln141Lys variant of ABCG2 was only subtly different in terms of export of chemotherapeutic drugs compared with wild-type ABCG2 (Tamura et al., 2007), which emphasizes that studies on the impact of SNPs on ABCG2 function have to be taken Apo-A1 HDL sitosterol lipid droplets urate lumen ABCG2 ABCG5/G8 Apo-A1 HDL sitosterol lipidpp droplets urate lumen ABCG2 ABCG5/G8 lumen ABCG5/G8 sitosterol Figure 2 Principal functions of human ABCG transporters. Login to comment 182 ABCG5 p.Arg50Cys The former identified a single locus effect of SNP rs4245791 (in intron 3 of the ABCG8) on total cholesterol levels, while the latter identified rs6756629 (resulting in an Arg50Cys change in ABCG5) as being associated with both raised total and low density lipoprotein-cholesterol. Login to comment