Dual Tyrosyl-DNA Phosphodiesterase/Topoisomerase Inibitors
Purdue University researchers have developed a series of novel, low molecular-weight compounds that can act as dual inhibitors of both TOP1 and TDP1. A dual inhibitor of this type would offer significant advantages over individual TOP1 and TDP1inhibitors alone such as simplification of delivery and bioavailability. In lab tests, the dual inhibitor is an equally potent TOP1 inhibitor as the commercially available camptothecin. These molecules are thought to function by stalling the DNA synthesis phase of the cell cycle, thereby inducing apoptosis, and effectively killing the cell. This drug could work in combination with other chemotherapies to effectively eliminate highly proliferative cell growth in the body.
First dual inhibitor of TOP1 and TDP1Shown to be as cytotoxic to TOP1 as camptothecinA potentially more potent chemotherapy agent
Cancer TreatmentMedical/HealthcarePharmaceuticals
Mark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
United States
8,912,213
美国
