Publications by authors named "Maria Gaetana Moschella"
Article Synopsis
- Thymidylate synthase (TS) is important for DNA synthesis and repair, and its overexpression contributes to drug resistance in cancer cells, particularly in ovarian and colon cancers.
- This study found that novel TS dimer disrupters (Ddis) were more effective at killing cancer cells when used alongside inhibitors of drug efflux proteins, which prevent the drugs from leaving the cells.
- The research also utilized a protein transfection agent to enhance the uptake of these Ddis, leading to reduced TS protein levels and disruptions in the cell cycle, indicating potential for improved cancer therapies.
Drugs that target human thymidylate synthase (hTS), a dimeric enzyme, are widely used in anticancer therapy. However, treatment with classical substrate-site-directed TS inhibitors induces over-expression of this protein and development of drug resistance. We thus pursued an alternative strategy that led us to the discovery of TS-dimer destabilizers.
View Article and Find Full Text PDF