This technology identifies a class of small molecules that inhibit DNA synthesis in plasmodium falciparum.
Malaria is the cause of a global health crisis that affects 500 million people worldwide each year. Unfortunately, the most prevalent parasite that causes malaria, Plasmodium falciparum, is adaptive and readily develops drug resistance. As a result, resistance to artemisinin-based combination therapy (ACT), the current frontline treatment for malaria, has been documented in Southeast Asia and is expected to spread rapidly and diminish its efficacy. As such, there is a growing need for new antimalarial therapies.
This technology describes a class of small molecules that have direct inhibition on DNA synthesis in Plasmodium falciparum. Using a high-throughput screen, this technology identified several inhibitors of the protein Equilibrative Nucleoside Transporter 1 (PfENT1), a protein that facilitates nucleoside uptake into the parasite. The identified antimalarial compounds could be used to treat malaria infection and prevent the spread of resistant strains.
The identified PfENT1 inhibitors have been demonstrated to inhibit P. falciparum growth in culture.
Patent Pending (US 20160122362)
IR CU13311
Licensing Contact: Jerry Kokoshka