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10.1186/s13104-015-1405-4 http://scihub22266oqcxt.onion/10.1186/s13104-015-1405-4 C4587578!4587578!26415506     free     free     free Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       BMC+Res+Notes 2015 ; 8 (ä): ä Nephropedia Template TP {{tp|p=26415506|t=2015. ABCG2 impairs the activity of the aurora kinase inhibitor tozasertib but not of alisertib |pdf=|usr=}}{{26415506}} gab.com Text ABCG2 impairs the activity of the aurora kinase inhibitor tozasertib but not of alisertib JO: BMC Res Notes http://www.kidney.de/pget.php?&tw=1&pmid=26415506 #FOAvip Background: Recently, we have shown that the ATP-binding cassette (ABC) transporter ABCB1 interferes with the anti-cancer activity of the pan-aurora kinase inhibitor tozasertib (VX680, MK-0457) but not of the aurora kinase A and B inhibitor alisertib (MLN8237). Preliminary data had suggested tozasertib also to be a substrate of the ABC transporter ABCG2, another ABC transporter potentially involved in cancer cell drug resistance. Here, we studied the effect of ABCG2 on the activity of tozasertib and alisertib. Results: The tozasertib concentration that reduces cell viability by 50 % (IC50) was dramatically increased in ABCG2-transduced UKF-NB-3ABCG2 cells (48.8-fold) compared to UKF-NB-3 cells and vector-transduced control cells. The ABCG2 inhibitor WK-X-34 reduced tozasertib IC50 to the level of non-ABCG2-expressing UKF-NB-3 cells. Furthermore, ABCG2 depletion from UKF-NB-3ABCG2 cells using another lentiviral vector expressing an shRNA against the bicistronic mRNA of ABCG2 and eGFP largely re-sensitised these cells to tozasertib. In contrast, alisertib activity was not affected by ABCG2 expression. Conclusions: Tozasertib but not alisertib activity is affected by ABCG2 expression. This should be considered within the design and analysis of experiments and clinical trials investigating these compounds. Electronic supplementary material: The online version of this article (doi:10.1186/s13104-015-1405-4) contains supplementary material, which is available to authorized users. Twit Text FOAVip ABCG2 impairs the activity of the aurora kinase inhibitor tozasertib but not of alisertib ????BMC Res Notes http://www.kidney.de/pget.php?&tw=1&pmid=26415506 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=26415506 #FOAvip English Wikipedia <ref>{{Cite pmid|26415506}}</ref> ABCG2 impairs the activity of the aurora kinase inhibitor tozasertib but not of alisertib #MMPMID26415506 Michaelis M; Selt F; Rothweiler F; Wiese M; Cinatl J BMC Res Notes 2015[]; 8 (ä): ä PMID26415506show ga Background: Recently, we have shown that the ATP-binding cassette (ABC) transporter ABCB1 interferes with the anti-cancer activity of the pan-aurora kinase inhibitor tozasertib (VX680, MK-0457) but not of the aurora kinase A and B inhibitor alisertib (MLN8237). Preliminary data had suggested tozasertib also to be a substrate of the ABC transporter ABCG2, another ABC transporter potentially involved in cancer cell drug resistance. Here, we studied the effect of ABCG2 on the activity of tozasertib and alisertib. Results: The tozasertib concentration that reduces cell viability by 50 % (IC50) was dramatically increased in ABCG2-transduced UKF-NB-3ABCG2 cells (48.8-fold) compared to UKF-NB-3 cells and vector-transduced control cells. The ABCG2 inhibitor WK-X-34 reduced tozasertib IC50 to the level of non-ABCG2-expressing UKF-NB-3 cells. Furthermore, ABCG2 depletion from UKF-NB-3ABCG2 cells using another lentiviral vector expressing an shRNA against the bicistronic mRNA of ABCG2 and eGFP largely re-sensitised these cells to tozasertib. In contrast, alisertib activity was not affected by ABCG2 expression. Conclusions: Tozasertib but not alisertib activity is affected by ABCG2 expression. This should be considered within the design and analysis of experiments and clinical trials investigating these compounds. Electronic supplementary material: The online version of this article (doi:10.1186/s13104-015-1405-4) contains supplementary material, which is available to authorized users. äABCG2 impairs the activity of the aurora kinase inhibitor tozasertib b(epmc).pdf DeepDyve Pubget Overpricing