Back to Search
Start Over
PBK/TOPK inhibitor OTS964 resistance is mediated by ABCB1-dependent transport function in cancer: in vitro and in vivo study.
- Source :
- Molecular Cancer; 2/8/2022, Vol. 21 Issue 1, p1-6, 6p
- Publication Year :
- 2022
-
Abstract
- Highlights: 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14764598
- Volume :
- 21
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Molecular Cancer
- Publication Type :
- Academic Journal
- Accession number :
- 155123706
- Full Text :
- https://doi.org/10.1186/s12943-022-01512-0