ABCMdb

ABCG2 p.Pro501Ala

None has been submitted yet.

Publications

PMID: 21854076 [PubMed] Ni Z et al: "Identification of proline residues in or near the transmembrane helices of the human breast cancer resistance protein (BCRP/ABCG2) that are important for transport activity and substrate specificity."

No. Sentence Comment

46 Full-length wild-type human BCRP cDNA in pcDNA3.1 was subcloned into pcDNA5/ FRT.15 The pcDNA5/FRT plasmid containing full-length human BCRP cDNA was used as a template to generate all the BCRP mutants using PCR mutagenesis as previously described.15 The following forward primers were used for mutagenesis: P392A (5'-AAC TTG CTG GGT AAT GCC CAG GCC TCT ATA GCT C-3'), P480A (5'-CTG TTA TCT GAT TTA TTA GCC ATG AGG ATG TTA CCA AG-3'), P485A (5'-CCC ATG AGG ATG TTA GCA AGT ATT ATA TTT ACC TGT ATA G-3'), P501A (5'-CAT GTT AGG ATT GAA GGC AAA GGC AGA TGC CTT C-3'), P574A (5'-CAG TAC TTC AGC ATT GCA CGA TAT GGA TTT ACG-3'), and P623A (5'-GGC ATC GAT CTC TCA GCC TGG GGC TTG TGG AAG AAT-3'). Login to comment
104 The estimated relative cell surface expression levels of wild-type and mutant BCRP based on the differences in median fluorescence between 5D3 and IgG2b control incubations were 100 ± 22, 108 ± 4, 89 ± 1, 139 ± 32, 75 ± 16, 76 ± 9, and 114 ± 0.7% for three independent determinations for wild-type BCRP, P392A, P480A, P485A, P501A, P574A, and P623A, respectively. Login to comment
129 The pcDNA5 vector control, wild-type BCRP, P392A, P480A, P485A, P501A, P574A, and P623A are indicated by P, WT, 392, 480, 485, 501, 574, and 623, respectively. Login to comment
132 Drug Resistance Profile of Wild-Type and Mutant BCRPa MX SN-38 Dox Rho123 IC50 (nM) RR IC50 (nM) RR IC50 (nM) RR IC50 (nM) RR pcDNA5/FRT 5.6 ± 0.8 - 1.7 ± 0.1 - 33.1 ± 2.2 - 4218 ± 400.0 - wild-type BCRP 51.5 ± 8.5 9.2 30.3 ± 2.0 17.8 40.9 ± 6.7 1.2 4446 ± 261.5 1.1 P392A 24.6 ± 3.8 4.4* 13.1 ± 1.0 7.7* 34.8 ± 1.7 1.1 5326 ± 414.1 1.3 P480A 69.4 ± 10.5 12.4 37.8 ± 1.5 22.2 29.0 ± 4.0 0.9 5107 ± 272.7 1.2 P485A 38.5 ± 7.0 6.9 15.9 ± 2.6 9.4* 41.8 ± 5.3 1.3 3237 ± 199.5 0.8 P501A 40.9 ± 14.6 7.3 27.5 ± 2.4 16.2 23.2 ± 3.8 0.7 4480 ± 816.4 1.1 P574A 49.6 ± 12.5 8.9 32.5 ± 2.6 19.1 29.6 ± 3.5 0.9 5320 ± 419.8 1.3 P623A 68.4 ± 14.4 12.2 36.8 ± 2.8 21.6 37.0 ± 8.8 1.1 3302 ± 388.1 0.8 a The relative resistance (RR) values represent the relative levels of resistance of the mutants compared to that of wild-type BCRP and were calculated by dividing the IC50 values of wild-type and mutant BCRP by the IC50 values of the vector control. Login to comment