ABCB1 overexpression significantly desensitized both drug-selected and gene-transfected cells, which overexpress ABCB1, to OTS964 and that this drug resistance can be antagonized by verapamil, a known ABCB1 inhibitor. Consistently, a similar trend was observed in tumor-bearing mice.OTS964 stimulated ATPase activity of ABCB1 and upregulated expression levels of ABCB1, resulting in induced resistance to other ABCB1 substrate-drugs, such as paclitaxel.OTS964 received a comparable affinity score and can dock into the substrate-binding site of human ABCB1 protein.
CITATION STYLE
Yang, Y., Teng, Q. X., Wu, Z. X., Wang, J. Q., Lei, Z. N., Lusvarghi, S., … Chen, Z. S. (2022, December 1). PBK/TOPK inhibitor OTS964 resistance is mediated by ABCB1-dependent transport function in cancer: in vitro and in vivo study. Molecular Cancer. BioMed Central Ltd. https://doi.org/10.1186/s12943-022-01512-0
Mendeley helps you to discover research relevant for your work.