ABCMdb

ABCG2 p.Arg482Tyr

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Publications

PMID: 14566825 [PubMed] Miwa M et al: "Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants."

No. Sentence Comment

63 PA/WT2 (R482) and PA/R482Y (Group 1) showed higher degrees of resistance to SN-38 than to mitoxantrone. Login to comment
104 These 13 PA/R482X2 and PA/R482Y cells exhibited significantly greater resistance to doxorubicin than PA/WT2. Login to comment
160 Group 1 member transfectants (PA/WT and PA/R482Y) showed higher degrees of resistance to SN-38 than to mitoxantrone. Login to comment

PMID: 15670731 [PubMed] Ozvegy-Laczka C et al: "Single amino acid (482) variants of the ABCG2 multidrug transporter: major differences in transport capacity and substrate recognition."

No. Sentence Comment

48 The two internal complementary primer pairs containing the specific mutation were: 5V-tta tta cca atg atc atg tta cc-3Vand 5-Vgg taa cat gat cat tgg taa taa-3V (R482I), 5V-tta tca gat cta tta ccc atg-3Vand 5V-gg taa cat cat cat ggg taa t-3V(R482M), 5V-ta ccc atg tcg atg tta cca a-3Vand 5V-t tgg taa cat cga cat ggg ta-3V(R482S), 5V-cc atg gac atg tta cca tcg att ata-3V and 5V-tat aat cga tgg taa cat gtc cat gg-3V (R482D), 5V-atg tta cca tcg att ata ttt acc-3Vand 5V-cc atg aat atg tta cca tcg att ata-3V (R482N), 5V-tta tta cct atg aag atg tta-3V cc and 5V-gg taa cat ctt cat agg taa taa-3V(R482K) and 5V-tta tta cct atg tac atg tta cc-3Vand 5V-gg taa cat gta cat agg taa taa-3V (R482Y). Login to comment
159 We found that while the R482K, R482Y, the wtABCG2, and the inactive K86M mutant had no R123 extrusion activity, several ABCG2 variants were highly active in R123 extrusion. Login to comment
198 While the wtABCG2, the R482K and R482Y mutants are already fully activated, and prazosin either does not affect or reduces the ATPase activity, the other variants can be further stimulated by exogenously added substrates. Login to comment
209 The exceptions were the R482Y mutant, effective only in mitoxantrone transport, and the R482K mutant, showing no transport activity with any of these substrates. Login to comment
216 Actually, the R482K mutant showed no measurable transport activity in any of the assays applied here, while the R482Y was found to be active only in the whole-cell mitoxantrone extrusion assay (see Fig. 4A). Login to comment
226 We found that the R482Y mutant is a very weak mitoxantrone transporter (see Fig. 4A), and Miwa et al. [27] demonstrated that this mutant confers decreased resistance in murine cells against MX. Login to comment

PMID: 16815914 [PubMed] Ejendal KF et al: "The nature of amino acid 482 of human ABCG2 affects substrate transport and ATP hydrolysis but not substrate binding."

No. Sentence Comment

7 Six of the mutants (R482G, R482H, R482K, R482P, R482T, and R482Y) and the wild-type protein (R482wt) were selected for studies of basal and stimulated ATPase activity and photoaffinity labeling with the substrate analog [125 I]iodoarylazidoprazosin. Login to comment
69 Transport of the fluorescent compound Bodipy FL prazosin followed a similar pattern to that observed for rhodamine 123, where the variants R482wt, R482K, R482H, and R482Y show the least transport (Fig. 3). Login to comment
71 Analysis of the substrate binding properties of wild-type and six mutant ABCG2 proteins In order to further investigate the effects of the R482X mutations, we studied the drug-binding ability of a selection of ABCG2 mutants (R482G, R482H, R482K, R482P, R482T, and R482Y) and the wild-type ABCG2 (R482wt). Login to comment
73 We selected mutants R482H, R482P, and R482Y because they are partially deficient in rhodamine 123 transport, whereas mitoxantrone transport is intact. Login to comment
86 We analyzed expression of ABCG2 in the membranes using the monoclonal antibody BXP-21 (Fig. 5A), which shows that the R482G, R482wt, and R482T membranes used here express less ABCG2, compared with the membranes expressing the R482H, R482K, R482P, and R482Y variants. Login to comment
90 In contrast, the R482H, R482K, R482Y, and R482wt variants are not markedly affected by the addition of 20 mM prazosin. Login to comment
96 Specific [125 I]IAAP photoaffinity labeling of crude membranes derived from HeLa cells expressing wild-type ABCG2 (R482wt) and the ABCG2 variants R482G, R482H, R482K, R482P, R482T, and R482Y. Login to comment
106 Basal and drug-stimulated ATPase activity of wild-type ABCG2 (R482wt) and ABCG2 variants R482G, R482H, R482K, R482P, R482T, and R482Y. Login to comment
139 It has previously been suggested for the R482Y variant that unknown endogenous substrates already fully stimulate the basal activity, which cannot be further stimulated by added exogenous substrates like prazosin (O¨ zvegy-Laczka et al. 2005a). Login to comment
141 Moreover, several variants (R482H, R482K, R482wt, and R482Y) showed no prazosin-stimulated ATPase activity. Login to comment

PMID: 17015488 [PubMed] Sarkadi B et al: "Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system."

No. Sentence Comment

811 Rhodamine-123 was extruded by most of the mutants, except by R482K, R482Y, and the wild-type ABCG2. Login to comment

PMID: 24384916 [PubMed] Telbisz A et al: "Regulation of the function of the human ABCG2 multidrug transporter by cholesterol and bile acids: effects of mutations in potential substrate and steroid binding sites."

No. Sentence Comment

108 Similar to earlier findings, there was a well-measurable Ko143-sensitive Hst dye transport both in the cells expressing wtABCG2 and in those expressing most R482 mutants, with only very low activity in the case of the R482K and R482Y variants (Fig. 1B). Login to comment

PMID: 25036722 [PubMed] Szafraniec MJ et al: "Determinants of the activity and substrate recognition of breast cancer resistance protein (ABCG2)."

No. Sentence Comment

172 Rhodamine was effluxed by most of these variants except for Arg482 Lys, Arg482 Tyr and WT protein. Login to comment
173 Arg482 Lys and Arg482 Tyr did not drive out Hoechst 33342 either (O &#a8; zvegy-Laczka et al., 2005). Login to comment