ABCMdb

PMID: 19135105

Hegedus C, Szakacs G, Homolya L, Orban TI, Telbisz A, Jani M, Sarkadi B
Ins and outs of the ABCG2 multidrug transporter: an update on in vitro functional assays.
Adv Drug Deliv Rev. 2009 Jan 31;61(1):47-56. Epub 2008 Dec 24., 2009-01-31 [PubMed]

Sentences

No. Mutations Sentence Comment

975 ABCG2 p.Arg482Gly WhileR482 is thewild-type form of ABCG2, R482G and R482Twere suggested to be gain-of-function mutations acquired during the course of drug selection. Login to comment 978 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly In contrast, doxorubicin and rhodamine123 are transported by the R482G and R482T protein variants, whereas they are not substrates for wtABCG2 [11,19,23,24]. Login to comment 983 ABCG2 p.Gln141Lys C421A, resulting in the Q141K amino acid change, has been examined most extensively, due to its high frequency in Asian and Caucasian populations [27,28]. Login to comment 1061 ABCG2 p.Arg482Thr Importantly, [(3)H]azidopine can covalently link to both wtABCG2 and to the ABCG2 R482T mutant variant. Login to comment 1174 ABCG2 p.Lys86Met After transient transfection of cells with plasmids expressing GFP-ABCG2 or the nonfunctional GFP-ABCG2 K86M mutant protein, the fluorescent fusion species were found to be well-suited for rapid flow cytometry or fluorescence microscopy applications [102]. Login to comment 1178 ABCG2 p.Lys86Met Using a specific inhibitor, either Ko143 or FTC [10], and comparing the results with those of the GFP-tagged K86M species, the transport characteristics of the applied fluorescent drug can be rapidly and reliably assessed. Login to comment 1196 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly In contrast, Sf9 membranes engineered to overexpress the ABCG2 R482G or ABCG2 R482T mutants show much higher substrate stimulation. Login to comment 1210 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly Interestingly, the substrate-stimulated ATPase activity of the ABCG2 R482G and ABCG2 R482T mutant variants cannot be further increased by cholesterol loading. Login to comment