1 results match your criteria: "Tianjin Medical University Tianjin 300070 China xujingyuan@tmu.edu.cn.[Affiliation]"
Pt(iv) derivatives of cisplatin and oxaliplatin bearing an EMT-related TMEM16A/COX-2-selective dual inhibitor against colorectal cancer cells HCT116.
RSC Med Chem
August 2024
Department of Chemical Biology and Tianjin Key Laboratory of Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University Tianjin 300070 China
Article Synopsis
- - Colorectal cancer exhibits over-expression of TMEM16A and COX-2, which creates an opportunity for targeted treatments.
- - Two new platinum (Pt(iv)) drug conjugates, complexes 1 and 2, were developed to enhance the efficacy of existing drugs such as cisplatin and oxaliplatin, with complex 2 showing higher toxicity against cancer cells.
- - Complex 2 demonstrated a significantly greater ability to kill colorectal cancer cells (22-fold increase) and showed better selectivity towards cancer cells compared to normal cells, working by triggering multiple biological pathways involved in cancer progression.