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Elevated ABCB1 Expression Confers Acquired Resistance to Aurora Kinase Inhibitor GSK-1070916 in Cancer Cells.
Wu ZX, Yang Y, Wang JQ, Zhou WM, Chen J, Fu YG, Patel K, Chen ZS, Zhang JY. Wu ZX, et al. Front Pharmacol. 2021 Jan 14;11:615824. doi: 10.3389/fphar.2020.615824. eCollection 2020. Front Pharmacol. 2021. PMID: 33519482 Free PMC article.
In the present study, we revealed that the Aurora kinase inhibitor GSK-1070916 is a substrate of ABCB1. GSK-1070916 is a newly developed inhibitor that is currently under clinical investigation. ...GSK-1070916 concentration-dependently st …
In the present study, we revealed that the Aurora kinase inhibitor GSK-1070916 is a substrate of ABCB1. GSK-1070916 …
Leishmania donovani Aurora kinase: A promising therapeutic target against visceral leishmaniasis.
Chhajer R, Bhattacharyya A, Didwania N, Shadab M, Das N, Palit P, Vaidya T, Ali N. Chhajer R, et al. Biochim Biophys Acta. 2016 Sep;1860(9):1973-88. doi: 10.1016/j.bbagen.2016.06.005. Epub 2016 Jun 8. Biochim Biophys Acta. 2016. PMID: 27288586
Interestingly, the cell-cycle progressed unhindered, despite treatment with GSK-1070916 or Barasertib, inhibitors with greater potencies for the ATP-binding pocket compared to Hesperadin, which at nanomolar concentrations, severely compromised viability at IC50s 105 …
Interestingly, the cell-cycle progressed unhindered, despite treatment with GSK-1070916 or Barasertib, inhibitors with greater …
Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs.
Uitdehaag JC, de Roos JA, van Doornmalen AM, Prinsen MB, Spijkers-Hagelstein JA, de Vetter JR, de Man J, Buijsman RC, Zaman GJ. Uitdehaag JC, et al. PLoS One. 2015 May 27;10(5):e0125021. doi: 10.1371/journal.pone.0125021. eCollection 2015. PLoS One. 2015. PMID: 26018524 Free PMC article.
The EGFR/ERBB2 inhibitor neratinib acted synergistically with the spindle poison docetaxel and with the Aurora kinase inhibitor GSK-1070916 in cell lines with MYC amplification. Our approach can therefore efficiently discover novel drug combinations that selectively …
The EGFR/ERBB2 inhibitor neratinib acted synergistically with the spindle poison docetaxel and with the Aurora kinase inhibitor GSK- …
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D. Adams ND, et al. J Med Chem. 2010 May 27;53(10):3973-4001. doi: 10.1021/jm901870q. J Med Chem. 2010. PMID: 20420387
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