Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated Multidrug Resistance in Cancer Cells

In conclusion, MET/SMO dual inhibitor Glesatinib antagonized P-gp mediated MDR by inhibiting its efflux functions. This work provided important information for further clinical trials. Author Contributions QC and Z-SC: conception and design. QC, C-YC, H-LG, NJ, SS, SA, and Z-SC: development of methodology. QC, C-YC, H-LG, PG, and NJ: acquisition of data. QC, C-YC, H-LG, NJ, and Z-SC: analysis and interpretation of data. QC, C-YC, LR, YY, D-HY, and Z-SC: writing, review, and/or revision of the manuscript. All authors read and approved the final manuscript. Conflict of Interest Statement The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. Acknowledgments We thank Dr. Stephen Aller for providing the human ABCB1 homology model. We thank Dr. Tanaji T. Talele for providing the computing resources for the docking study. We thank Drs. Susan E. Bates and Robert W. Robey (NCI, NIH, Bethesda, MD) for providing the cell lines. We thank the support of Guangzhou Postdoctoral Foundation of International Training for QC and NIH funding (No. 1R15GM116043-01) to Z-SC. References 1. Housman G, Byler S, Heerboth S, Lapinska K, Longacre M, Snyder N, et al. Drug resistance in cancer: an overview. Cancers. (2014) 6:1769–92. doi: 10.3390/cancers6031769 PubMed Abstract | CrossRef Full Text | Google Scholar 2. Shukla S, Chen ZS, Ambudkar SV. Tyrosine kinase i...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research