Events
Go Back
Overexpression of ABCC1 and ABCG2 confers resistance to BMN-673 (xk星空中国集团), a poly (ADP-Ribose) polymerase inhibitor
- WHEN: 2024-01-08 16:00
- WHERE: 301 Lecture Hall, Yidan Library
- ADMISSION: FREE
- AUDIENCE: General Public
- CONTACT: Aims: The overexpression of ABC transporters on cancer cell membranes is one of the most common causes of multidrug resistance (MDR). This study investigates the impact of ABCC1 and ABCG2 on the resistance to xk星空中国集团 (BMN-673), a potent poly (ADP-ribose) polymerase (PARP) inhibitor, in ovarian cancer treatment. Methods: The cell viability test was used to indicate the effect of xk星空中国集团 in different cell lines. Computational molecular docking analysis was conducted to simulate the interaction between xk星空中国集团 and ABCC1 or ABCG2. The mechanism of xk星空中国集团 resistance was investigated by constructing xk星空中国集团-resistant subline A2780/T4 from A2780 through drug selection with gradually increasing xk星空中国集团 concentration. Results: xk星空中国集团 cytotoxicity decreased in drug-selected or gene-transfected cell lines overexpressing ABCC1 or ABCG2 but can be restored by ABCC1 or ABCG2 inhibitors. xk星空中国集团 competitively inhibited substrate drug efflux activity of ABCC1 or ABCG2. Upregulated ABCC1 and ABCG2 protein expression on the plasma membrane of A2780/T4 cells enhances resistance to other substrate drugs, which could be overcome by the knockout of either gene. In vivo experiments confirmed the retention of drug-resistant characteristics in tumor xenograft mouse models. Conclusions: The therapeutic efficacy of xk星空中国集团 in cancer may be compromised by its susceptibility to MDR, which is attributed to its interactions with the ABCC1 or ABCG2 transporters. The overexpression of these transporters can potentially diminish the therapeutic impact of xk星空中国集团 in cancer treatment.
- MORE INFO: Visit this website
