PMID: 26351135

Darby RA, Unsworth A, Knapp S, Kerr ID, Callaghan R
Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors.
Cancer Chemother Pharmacol. 2015 Oct;76(4):853-64. doi: 10.1007/s00280-015-2858-9. Epub 2015 Sep 9., [PubMed]
Sentences
No. Mutations Sentence Comment
152 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 26351135:152:1210
status: NEW
view ABCG2 p.Arg482Gly details
 Statistical comparisons were made using ANOVA, with the Bartlett`s post hoc test Cytotoxic drug Cell line Chemosensitisation agent Control FTC 0.3 bc;M K00135 0.1 bc;M K00135 0.3 bc;M K00486 0.3 bc;M K00486 1.0 bc;M Flavopiridol MCF7 52.6 &#b1; 7.3 42.7 &#b1; 5.9 57.7 &#b1; 4.6 52.7 &#b1; 5.9 44.7 &#b1; 6.6 40.4 &#b1; 5.3 MCF7FLV1000 2017 &#b1; 78 193 &#b1; 30* 728 &#b1; 87* 201 &#b1; 20* 347 &#b1; 24* 153 &#b1; 11* Resistance 38.3 4.5 12.6 3.8 7.8 3.8 Mitoxantrone MCF7 12.9 &#b1; 3.1 5.9 &#b1; 1.9 8.7 &#b1; 1.8 6.2 &#b1; 0.9 6.3 &#b1; 2.9 6.4 &#b1; 1.7 MCF7FLV1000 525 &#b1; 69 86 &#b1; 4* 209 &#b1; 51* 81 &#b1; 21* 174 &#b1; 49* 35 &#b1; 12* Resistance 40.7 15.5 24.1 13.1 27.4 5.4 Topotecan MCF7 8.1 &#b1; 1.3 4.5 &#b1; 0.4 6.3 &#b1; 0.7 5.2 &#b1; 0.5 6.8 &#b1; 1.1 4.9 &#b1; 0.8 MCF7FLV1000 2736 &#b1; 127 163 &#b1; 27* 1315 &#b1; 86* 353 &#b1; 32* 571 &#b1; 15* 177 &#b1; 13* Resistance 336 35.9 210 68.1 83.6 35.8 Doxorubicin MCF7 8.5 &#b1; 0.8 9.0 &#b1; 1.2 11.1 &#b1; 0.52 6.6 &#b1; 0.6 12.8 &#b1; 2.1 9.7 &#b1; 1.1 MCF7FLV1000 69.9 &#b1; 6.9 29.8 &#b1; 3.7 62.6 &#b1; 3.3* 34.7 &#b1; 4.8* 34 &#b1; 4.2* 24.5 &#b1; 3.6* Resistance 8.2 3.3 5.6 5.2 2.7 2.5 The well-characterised R482G mutant isoform of ABCG2 imparts a number of changes in the cross-resistance pattern compared to the wild-type isoform. Login to comment